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(+)-Niguldipine hydrochloride is an antagonist for calcium channel. (+)-Niguldipine hydrochloride produces vasodilation by blocking calcium channels and reducing the transmembrane influx of calcium ions. (+)-Niguldipine hydrochloride inhibits U-46619 (HY-108566)-induced coronary vasoconstriction in guineapig Langendorff heart with pID50 of 11.37, binds to calcium channel on guineapig skeletal muscle membrane with Ki of 9.75, and lowers the blood pressure in spontaneously hypertensive rat with pED30 of 7.1. (+)-Niguldipine hydrochloride ameliorates cardiovascular diseases such as hypertension, angina pectoris and arrhythmias .
L-772405 is a selective 5-HT1D receptor agonist with the Ki values of 318, 29 and ＞ 1000 nM aganist guineapig 5-HT1B receptor, guineapig 5-HT1D receptor and rat 5-HT rransporter, respectively. L-772405 decreases the potassium-induced outflow of 5-HT with an IC50 value of 240 nM .
Cyclic HPMPC is a potent antiviral agent. Cyclic HPMPC can increase arterial oxygen saturation levels in lethal vaccinia virus (IHD strain)-infected mice. Cyclic HPMPC improves the outcome of congenital guineapig cytomegalovirus (GPCMV) infection and decreases viral replication in guineapig model .
BMS-363131 is a selective inhibitor for tryptase, with an IC50 <1.7 nM. BMS-363131 is hydrolytic stable at pH=7 and pH=9. BMS-363131 attenuates the astham in a guineapig model .
Elbanizine inhibits histamine, bradykinin, histamin-release from rat mast cells (IC50 of 0.26 μM) and the IgE-mediated passive cutaneous anaphylaxis (PCA) reaction. Elbanizine exhibits antiallergic and antiasthmatic in guineapig model .
Istaroxime oxalate (PST2744 oxalate) is the oxalate form of Istaroxime (HY-15718). Istaroxime oxalate is is an inotropic agent, that inhibits Na +/K +-ATPase with an IC50 of 0.11 μM. Istaroxime oxalate increases force of contraction in guineapig atria and twitch amplitude in isolated guineapig myocytes without causing lethal arrhythmias .
Nyasicoside is a norlignan glucosides that can be isolated from Curculigo capitulate. Nyasicoside has potent activity against ouabain-induced arrhythmia in the heart preparations of guineapig .
Pirodomast (Sch 37224) is a leukotriene formation inhibitor. Pirodomast inhibits LTD4 andthromboxane B2 release by anaphylactic guineapig lung with the IC50 values of 3.9 and 1.9 μM, respectively. Pirodomast can be used for study of asthma .
Symetine dihydrochloride (L 16726 dihydrochloride) is the dihydrochloride form of Symetine (HY-101590). Symetine dihydrochloride exhibits antiprotozoal activity aginst Entamoeba histolytica, and ameliorates the amebic liver abscess in guineapig model .
SUN-1334H free base is an orally active inhibitor for histamine H1 receptor, with an IC50 of 20.3 nM and Ki of 9.7 nM. SUN-1334H free base inhibits histamine-induced contractions of isolated guinea-pig ileum with an IC50 of 0.198 μM. SUN-1334H free base inhibits histamine-induced bronchoconstriction in guineapigs, histamine-induced skin wheals in beagle dogs, and ovalbumin-induced rhinitis in guineapigs .
LY 292728 is a potent leukotriene B4 (LTB4) receptor antagonist. LY 292728 binds to human neutrophils with a Ki of 0.47 nM and binds to guineapig lung membranes with a Ki of 0.04 nM .
HSR-609 is an orally active amphoteric antiallergic agent. HSR-609 has a high affinity for histamine H1-receptor in the guineapig cerebral cortex. HSR-609 inhibits allergic airway hyperresponsiveness to Acetylcholine. HSR-609 shows poor ability to penetrate into the CNS in mice and guineapigs .
11-trans Leukotriene E4 is an isomer of Leukotriene E4 (LTE4). Slow isomerization of the C-11 double bond of LTE4 leads to the formation of 11-trans LTE4. 11-trans Leukotriene E4 is equipotent to LTE4 in contracting guineapig ileum .
RS-15385-198 is the enantiomer of Delequamine (RS-15385-197) (HY-106874). RS-15385-198 exhibits a pKi of 6.32 for α2-adrenoceptors in the rat cortex. RS-15385-198 is an antagonist for UK-14304 (HY-B0659) in the rat vas deferens and in the guinea-pig ileum .
JNJ-39729209 is an antagonist for transient receptor potential vanilloid 1 (TRPV1) with pIC50 of 7.9, 8.5, 7.9 and 7.7 for TRPV1 from human, rat, canine and guineapig. JNJ-39729209 inhibits Capsaicin (HY-10448)-induced hypotension and inhibit thereby hypothermia. JNJ-39729209 exhibits anti-inflammatory and analgesic activities in Carrageenan (HY-125474)- and CFA (HY-153808)-induced thermal hyperalgesia rat models. JNJ-39729209 exhibits anti-cough effects in guineapigs .
ZM260384 is a KATP channel opener that accelerates metabolism and inhibits the decline of guineapig isolated diaphragm function, thereby affecting muscle contraction. ZM260384 can be used to study muscle function under hypoxic conditions .
Scyliorhinin I is a tachykinin-1 (NK-1) and tachykinin-2 (NK-2) receptor agonist with a Ki value of 0.9 nM for rat submandibular gland NK-1 receptor and 2 nM for hamster bladder NK-2 receptor. Scyliorhinin I has the ability to contract the longitudinal muscles of the guineapig ileum .
R-96544 (free base) is a potent, selective and competitive 5-HT2 receptor antagonist. R-96544 (free base) inhibits platelet aggregation induced by serotonin, and inhibits 5-HT2A receptor-mediated contraction of guineapig trachea .
Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with Ki values of 12, 42 and 43 μM at the guineapig, rat and human neurokinin NK1 receptors, respectively .
SC-41930 is a orally active eukotriene-B4 receptor antagonist. SC-41930 alleviates inflammation in guineapig acetic acid-induced colonic inflammation model .
(Rac)-SC-31391, a prostaglandin analog, is a strong activator of the bladder muscle contractility that enhanced twitch responses elicited by field stimulation in the guineapig detrusor muscle. (Rac)-SC-31391 contracts human bladder muscle through the activation of PGF2α receptors .
CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guineapigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD) .
ONO-RS-347 is an orally active and potent antagonist of leukotriene C4 and D4. ONO-RS-347 inhibits LTD4-induced bronchoconstriction in guineapigs. ONO-RS-347 is promising for research of allergic asthma and other immediate hypersensitivty diseases .
AM 92016 is a potassium channel blocker. AM 92016 can increase the duration of action potentials in isolated ventricular cells from guineapigs and rabbits. AM 92016 has proarrhythmic activity in guineapigs and pigs .
Onitin is a natural product, that can be isolated from Onychium siliculosum. Onitin is also a non-competitive antagonist of histamine. Onitin shows activity in blocking the peristaltic reflex of the guinea-pig ileum, in inhibition of the responses of guinea-pig ileum to histamine and of inhibition of the responses of guinea-pig tracheal muscle to histamine .
PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca 2+ exchanger in guineapig airway smooth muscle .
GS 283 is a compound with calcium antagonist and weak histamine and muscarinic receptor blocking activity, with activity in modulating contraction of guineapig and rat tracheal smooth muscle. GS 283 inhibits contractions induced by carbachol, histamine (guineapig only), and high K? in guineapig and rat tracheal smooth muscle, inhibits Ca2?-induced contractions in guineapig tracheal smooth muscle, and at high concentrations completely abolishes contractions induced by carbachol in Ca2?-free medium.
AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guineapig cortex 5HT1B/1D and recombinant guineapig5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guineapig5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guineapig5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.
ReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guineapig brain) with Ki of 0.19±0.04 μM and the non-selective σ site (guineapig brain) with Ki of 0.45 μM.
16,16-Dimethylprostaglandin F2α (16,16-Dimethyl-PGF2α) is a potent analog of PGF2α (HY-12956), which exhibits similar binding potency as PGF2α does. 16,16-Dimethylprostaglandin F2α serves as a bronchoconstrictor .
Ro 3-1314 (9a,12a-Octadecadiynoic acid) is a plant lipoxygenase inhibitor. Ro 3-1314 is a linoleic acid metabolism inhibitor. Ro 3-1314 stimulates the antigen-induced contraction of guinea-pig tracheal spirals and the immunological release of slow reacting substance of anaphylaxis (SRS-A) from actively sensitized guinea-pig lung fragments .
Hetramine is a compound with antihistamine and antiallergic activity that prevents histamine-induced intestinal contractions as well as allergy and anaphylactic shock in guineapigs.
Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guineapig brain membranes.
Gigantol is a natural product that could be isolated from Cymbidium giganteum. Gigantol is a potent inhibitor of the spontaneous contractions of the guinea-pig ileum .
3-Methylxanthine, a xanthine derivative, is a cyclic guanosine monophosphate (GMP) inhibitor, with an IC50 of 920 μM on guinea-pig isolated trachealis muscle.
Helveticoside (Strophanthidin-digitoxoside) is a helveticosid, possesses an ED50 of 0.17 μM for isolated guinea-pig ileum. Helveticoside has anticancer effect .
Berlopentin (Diacetylsplenopentine) is an antiviral agent, and protects guineapigs from foot-and-mouth disease (FMD) infection. Berlopentin has immunostimulatory properties .
Melitidin is a flavanone glycoside, that can be isolated from Citrus grandis 'Tomentosa'. Melitidin shows a good antitussive effect on cough induced by citric acid in Guineapig .
PD 140376 is a potent antagonist for the cholecystokininB/gastrin receptor, with Ki values of 0.18 nM and 0.21 nM in guinea-pig cortex and gastric gland membranes, respectively .
HMR 1556, a chromanol derivative, is a potent IKs blocker with IC50s of 10.5 nM and 34 nM in canine and guineapig left ventricular myocytes, respectively .
Axelopran sulfate is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guineapig κ receptor, respectively.
Leumorphin, human is a potent kappa opioid receptor (κ opioid receptor) agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guineapig ileum .
11-trans Leukotriene D4 (11-trans LTD4) is a C-11 double bond isomer of LTD4. LTD4 undergoes slow temperature-dependent isomerization to 11-trans LTD4 during storage. 11-trans LTD4 retains about 10-25 % of the potency for contraction of guineapig ileum, trachea and parenchyma compared to LTD4. It exhibits an ED50 ranging between 12-60 nM for contraction of guineapig trachea.
Azimilide (NE-10064) dihydrochloride is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
Azimilide(NE-10064) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
Axelopran (TD-1211) is an opioid receptor antagonist with pKi values of 9.8, 8.8 and 9.9 for human recombinant μ and δ receptors and guineapig κ receptor, respectively.
Cularine is a compound that relaxes guineapig tracheal and human bronchial smooth muscle, inhibits contraction induced by a variety of contractile agents, and has nonspecific antispasmodic activity, and its activity is structure-related.
CGP37157 is a potent, selective inhibitor of Na +/Ca 2+ exchanger, inhibiting the Na +-induced Ca 2+-release from guinea-pig heart mitochondria, with an IC50 of 0.8 μM.
BN 50341 is an orally active anticalcic agent and a benzazepine derivative. BN 50341 decreases the in vivo electrically induced thrombus formation in rat or guinea-pig artery and can be utilized in cardiovascular research .
Z-335 sodium is an orally active thromboxane a2 (TXA2) receptor antagonist, with IC50 values of 29.9 nM and 32.5 nM for human and Guineapig platelets, respectively .
Prifelone (R 830; R 830T; S 16820) is a di-tert-butylphenol with anti-inflammatory and antioxidant activity. Prifelone inhibits guineapig lung oxygenase and bovine seminal vesicle cyclooxygenase .
Quinophthalone is a dye with distinctive greenish yellow color. Quinophthalone is used as coloring agents for various materials. Quinophthalone is a strong sensitizer in guineapigs, and its threshold concentration for induction and challenge is 10 ppm .
Withanoside V (Standard) is the analytical standard of Withanoside V. This product is intended for research and analytical applications. Withanoside V, a withanolide glycoside, exhibits inhibitory activity for tachyphylaxis to Clonidine in isolated guinea-pig ileum .
SB-216641A (SB-216641 hydrochloride) is a selective antagonist of 5-HT1B/D receptor. SB-216641A shows high affinity and selectivity for h5-HT1B receptors over h5-HT1D receptors. SB-216641A inhibits the function of SKF-99101H .
LAS191859 is an orally active, potent and selective CRTh2 antagonist with an IC50 of 9.58 nM against human CRTh2. LAS191859 can be used for the research of chronic asthma .
16,16-Dimethylprostaglandin E1 (16,16-dimethyl-PGE1) is a PGE1 (HY-B0131) analog, induces bronchoconstrict and vascular smooth muscle contractions and suppresses the indomethacin induced cellular elongation .
QWF Peptide (Compound 4a) is a substance P antagonist with an IC50 of 0.09 μM. QWF Peptide antagonizes the SP-induced contraction of isolated guineapig trachea strips with an IC50 of 4.7 μM .
AHR-5333 is a selective human blood neutrophil 5-lipoxygenase inhibitor. AHR-5333 exhibits potent, long-acting activity in rat and guineapig in vivo models of immediate hypersensitivity .
R 56865 is a cardiomyocyte protective agent that protects against digitoxin (Ouabain)-induced myocardial calcium overload. R 56865 has a protective effect against digitoxin-induced intoxication in guineapig papillary muscle .
Aminopotentidine is a histamine H2 receptor antagonist with KB values of 220 nM and 280 nM for human and guineapigH2 receptors, respectively. It can also serve as a precursor for the synthesis of [125I] iodo derivatives .
NPD9948 is an antitussive agent with antitussive activity in a guineapig antitussive test. Its half antitussive dose (AtD50) is 14.5 mg/kg and 22.6 mg/kg when injected intraperitoneally and orally, respectively.
RO5101576 is a potent LTB4 receptor antagonist with activity to inhibit LTB4-induced calcium mobilization and chemotaxis of human neutrophils. RO5101576 significantly attenuated LTB4-induced pulmonary eosinophilia in guineapigs. RO5101576 inhibited allergen- and ozone-induced pulmonary neutrophilia in nonhuman primates with efficacy comparable to that of budesonide. RO5101576 had no effect on LPS-induced neutrophilia in guineapigs and cigarette smoke-induced neutrophilia in mice and rats. RO5101576 performed well in toxicology studies and was well tolerated .
AQ-RA 741 is a potent and selective M 2 antagonist. AQ-RA 741 inhibits the vagally or agonist-induced bradycardia in rats, cats and guinea-pigs. AQ-RA 741 is used in bradycardiac disorders research .
[Pro34]Neuropeptide Y, porcine is a selective NPY receptor (Y1 receptor) agonist. [Pro34]Neuropeptide Y, porcine evokes vasoconstrictions in the guineapig caval vein .
rel-Aprikalim (rel-RP 52891) is the relative configuration of Aprikalim (HY-121183). Aprikalim (RP 52891), a potassium channel opener (KCO), activates ATP-sensitive K + (KATP) channels in guineapig ventricular myocytes .
Bepafant (Web2170) is a platelet-activating factor (PAF) antagonist that protects against anaphylactic lethality in active and passive anaphylaxis models in mice and guineapigs in a dose-dependent manner and attenuates bronchoconstriction and blood pressure changes in anaphylaxis.
AHR-5333 mandelate is a selective human blood neutrophil 5-lipoxygenase inhibitor. AHR-5333 mandelate exhibits potent, long-acting activity in rat and guineapig in vivo models of immediate hypersensitivity .
Lipoxin A5 is an eicosapentaenoic acid derived from pig white blood cells. Lipoxin A5 slowly contracted the guineapig lung parenchymal strips with a contractile force similar to that of LXA4 and LXB4.2, but LXA5 did not have the vasodilating effect on the aortic smooth muscle shown by LXA4 and LXB4.2 .
(-)-Niguldipine ((R)-Niguldipine) hydrochloride is a calcium channel antagonist. (-)-Niguldipine hydrochloride exerts a vasodilatory effect by blocking calcium channels and reducing the transmembrane influx of calcium ions. (-)-Niguldipine can inhibit U-46619 (HY-108566)-induced coronary artery contraction in guineapig Langendorff hearts (pID50 of 9.93), has high affinity for calcium channel binding sites on guineapig skeletal muscle membranes (Ki of 8.10), and lowers blood pressure in spontaneously hypertensive rats (pED30 of 5.55). (-)-Niguldipine hydrochloride can improve cardiovascular diseases such as hypertension, angina pectoris, and arrhythmias .
Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guineapig.
Nylidrin hydrochloride was an effective inhibitor of IgE-mediated release of histamine from passively sensitized rat peritoneal mast cells and human basophils, and of IgG1-mediated release of histamine from passively sensitized guineapig lung slices.
ICI-204448 is a κ-opioid agonist with limited access to the CNS, ICI-204448 can displace the binding of the kappa-opioid ligand 3H-bremazocine from guineapig cerebellum membranes .
AQ-RA 721 is a compound that can distinguish between the m4 and M2 sites and can be used to characterize muscarinic receptor subtypes, which is helpful for the study of its muscarinic receptor properties in guineapig uterine smooth muscle.
Etomoxir((R)-(+)-Etomoxir) sodium salt is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guineapig .
SDZ-MKS 492 (MKS 492) is a selective inhibitor of cyclic GMP-inhibited phosphodiesterase (type III PDE). SDZ-MKS 492 inhibits antigen- or platelet activating factor (PAF)-induced bronchoconstriction and allergic reactions in guineapigs and rats .
Azimilide-d8 (dihydrochloride) is the deuterium labeled Azimilide dihydrochloride. Azimilide Dihydrochloride (NE-10064 Dihydrochloride) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
Trifenagrel is a platelet aggregation inhibitor that inhibits the inducing effects of arachidonic acid (AA) and collagen. The ED50s of trifenagrel for inhibiting AA- and collagen-induced platelet aggregation in guineapigs were 1.4 mg/kg and 9.4 mg/kg, respectively .
P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guineapig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guineapig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect .
8-O-Acetylharpagide is an iridoid isolated from Ajuga reptans with antitumoral, antiviral, antibacterial, and anti-inflammatory activities. 8-O-Acetylharpagide also has a biological activity on isolated smooth muscle preparations from guineapig .
Conessine, a steroidal alkaloid, is a potent and selective histamine H3 receptor antagonist with Kis of 5.4, 6.0, 5.7 and 25 nM for human, dog, guineapig, and rat H H3 receptor, respectively. Anti-malarial activity .
Asobamast is a potent, orally active antiallergic agent that inhibits ige mediated passive pulmonary allergic responses in rats (ED50=4.7 mg/kg) and inhibits antigen-induced mediator release from sensitized guineapig lung fragments .
3-Methylxanthine (Standard) is the analytical standard of 3-Methylxanthine. This product is intended for research and analytical applications. 3-Methylxanthine, a xanthine derivative, is a cyclic guanosine monophosphate (GMP) inhibitor, with an IC50 of 920 μM on guinea-pig isolated trachealis muscle.
3-Methylxanthine-d3 is deuterated labeled 3-Methylxanthine (HY-50723). 3-Methylxanthine, a xanthine derivative, is a cyclic guanosine monophosphate (GMP) inhibitor, with an IC50 of 920 μM on guinea-pig isolated trachealis muscle.
ICI-204448 free acid is a κ-opioid agonist with limited access to the CNS, ICI-204448 free acid can displace the binding of the kappa-opioid ligand 3H-bremazocine from guineapig cerebellum membranes .
MF63 is a selective and orally active inhibitor of mPGES-1. MF63 reduces the accumulation of PGE2, relieves pyresis, hyperalgesia, and inflammatory pain by inhibiting mPGES-1 .
Ro 24-5913 (Cinalukast) is an orally active and potent LTD4 antagonist with an IC50 value of 6.4 nM. Ro 24-5913 can be used for the research of asthma .
11-deoxy Prostaglandin F1α (11-deoxy PGF1α) is an analog of prostaglandin F1α, exhibits side effects on intestines and causes the uterine contraction. 11-deoxy Prostaglandin F1α exhibits activity as vasopressor and bronchoconstrictor .
L694247 is a selective 5-HT1D agonist with the pIC50 values of 10.03, 8.64, 6.42, and 5.66 for 5-HT1D, 5-HT1A, 5-HT1C, and 5-HT1E receptors , respectively .
Rupatadine-d4 (fumarate) is a deuterium labeled Rupatadine fumarate. Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 μM(rabbit platelet membranes/guineapig cerebellum membranes)[1][2][3].
Ritolukast (Wy-48252) is an orally active aerosol leukotriene (LTD4/E4) receptor antagonist. Ritolukast can be used to inhibit the bronchoconstriction caused by aerosol LTD4 in guineapigs, with an ID50 of 0.5mg/kg .
CHF-6550 is an antagonist for muscarinic M3 receptor and an agonist for β2 adrenoceptor (MABA), with pKi of 9.3 and 10.6, respectively. CHF-6550 exhibits good hepatocyte clearance in rat models and good pharmacokinetic characteristics in guineapigs .
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors .
AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guineapig, and rat DP2, respectively.
FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modify the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guineapig atrium .
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guineapig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively .
Norbormide shows vasoconstrictor activity by blocking calcium channel. The activity of Norbormide is species- and tissue-specific, endothelium independent, and is restricted to the peripheral arteries of rat. Norbormide is also a toxicant, and the oral LD50s in mouse, hamster, guineapig and rabbit are 2250, 140, 620, and 1000 mg/kg .
Leukotriene B4 dimethyl amide, an immunomodulator, stimulates contraction of isolated guineapig lung entities. Leukotriene B4 (LTB(4)) also stimulates human neutrophil migration, and LTB(4) antagonists may have anti-inflammatory activity in inflammatory pathophysiology .
(S)-(+)-Etomoxir is the S enantiomer of Etomoxir (HY-50202). Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guineapig .
EP 171 is a TP receptor agonist and human platelet activator. EP 171 can induce constriction of guineapig trachea, and the constriction can be inhibited by the TP receptor antagonist EP 092. EP 171 binds to TP receptors on intact human platelets with an IC50 of 2.9 nM .
AM211 sodium is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guineapig, and rat DP2, respectively.
[D-Trp11]-Neurotensin, an analogue of Neurotensin (NT), is a selective antagonist of NT in perfused rat hearts but behaves as a full agonist in guineapig atria and rat stomach strips. [D-Trp11]-Neurotensin can inhibit NT-induced hypotension .
11-Deoxy prostaglandin E1 (AY-23578; Doproston B) is an analog of prostaglandin E1 (PGE1) with bronchodilator activity. 11-Deoxy prostaglandin E1 inhibits histamine-induced bronchoconstriction and causes relaxation of tracheal strips in isolated guineapigs .
TASP0412098 is an orally available, potent and selective CRTH2/DP2 antagonist with high binding affinity (IC50 2.1 nM) and functional activity (IC50 12 nM). TASP0412098 has the potential to suppress asthma in mouse and guineapig bronchial asthma models .
3-Methylxanthine- 13C4, 15N3 is the 13C-labeled and 15N-labeled 3-Methylxanthine. 3-Methylxanthine, a xanthine derivative, is a cyclic guanosine monophosphate (GMP) inhibitor, with an IC50 of 920 μM on guinea-pig isolated trachealis muscle.
L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guineapig stomach gastrin and brain CCK receptors .
RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC50=58 nM). RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel . RPR-260243 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
LY393558 is a potent and orally active inhibitor of the 5-HT transporter and an antagonist of 5-HT1B and 5-HT1D receptors. LY393558 increase the extracellular levels of 5-HT in mice model frontal cortex. LY393558 can be used for researching depression .
SR2640 (hydrochloride) is a potent and selective competitive leukotriene D4/leukotriene E4 antagonist. SR2640 can be used for researching the role of leukotrienes in human asthma .
Defibrase, deinagkistrodonacutus is a proteolytic enzyme extraction of Agkistrodon halys venom. Defibrase can be used for degradation of fibrinogen. Defibrase can exacerbate myosin-induced EAM (experimental autoimmune myositis). Defibrase can be used for degradation of fibrinogen. Defibrase is commonly used for research of acute ischemic cerebrovascular disease, thromboangiitis obliterans, deep phlebitis and sudden deafness .
FR173657 is an orally active bradykinin B2 receptor antagonist (IC50: 0.56, 1.5, 2.9 nM for pig, rat, human B2 receptor respectively). FR173657 (p.o.) inhibits BK-induced bronchoconstriction in guinea-pigs (ED50: 0.075 mg/kg). FR173657 (p.o.) also inhibits Carrageenin-induced paw oedema in mice (ED50: 6.8 mg/kg). FR173657 can be used for research of inflammatory disease .
GDC-6599 is an orally active TRPA1 inhibitor, with IC50 values of 5.3 nM in humans, 6.6 nM in rats, 9.3 nM in dogs, 7.2 nM in monkeys, and 15 nM in guineapigs. GDC-6599 can be used in the research of neuropathic pain and respiratory diseases such as asthma and chronic cough .
LY 163443 is a selective antagonist of leukotrienes D4 (LTD4) and E4 (LTE4). LY 163443 can antagonize LTD4-induced contractions of guineapig ileum, trachea, and lung parenchyma. LY 163443 also inhibits tracheal contractions to LTE4 .
Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guineapig. The Ki values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a Ki of 8.6 nM in guineapig. The Ki values of Spiradoline mesylate for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline mesylate has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .
L-687306 is a high affinity muscarinic M1 receptor partial agonist with activity as a partial agonist of M1 receptors in rat ganglia and as a high affinity competitive antagonist at guineapig cardiac M2 and ileal M3 muscarinic receptors, useful for studying the receptor reserve of muscarinic receptors.
Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes . Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells .
JMV 449 is a potent neurotensin receptor agonist. JMV 449 shows an IC50 of 0.15 nM for inhibition of [ 125I]-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 has highly potent and long-lasting hypothermic and analgesic effects in the mouse .
JMV 449 acetate is a potent neurotensin receptor agonist. JMV 449 acetate shows an IC50 of 0.15 nM for inhibition of 125I-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 acetate has highly potent and long-lasting hypothermic and analgesic effects in the mouse .
FK888 is a potent, selective, and high affinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration .
Gardneramine is an orally active alkaloid that acts like papaverine. Gardneramine has peripheral vascular diastolic effect, direct inhibition on myocardium and central inhibition. Gardneramine showed antihypertensive, vasodilatation and atrial inhibition effects in rabbit, dog and guineapig models, respectively. Gardneramine also inhibits the movement of smooth muscle organs such as the stomach and intestines .
Piprofurol is a calcium channel inhibitor. Piprofurol inhibits the calcium-induced contractions in isolated potassium depolarized preparations of rat aorta in a concentration-dependent manner and relaxes the K +-induced contraction of the dog coronary artery and the rabbit basilar artery. Piprofurol exerts a negative inotropic effect on guinea-pig papillary muscle, with the EC50 of 5 μM .
KY 234 is an orally effective inhibitor that targets thromboxane A2 production, with an IC50 of 5 μM. KY 234 significantly inhibits leukotriene D4 (LTD4), histamine, and antigen-induced bronchoconstriction in guineapigs, with IC50 values of 6.0 mg/kg, 2.5 mg/kg, and 6.3 mg/kg, respectively .
Conessine dihydrobromide is a steroidal alkaloid and an effective, selective histamine H3 receptor antagonist with Ki values of 5.4, 6.0, 5.7, and 25 nM for human, dog, guineapig, and rat H3 receptors, respectively. Conessine dihydrobromide exhibits antimalarial activity and can be used in infection-related research .
Milveterol is a long-acting β(2)-adrenoceptor agonist with high binding activity. Milveterol exhibits high potency in vitro and a prolonged duration of action in a guineapig bronchoprotection model. Milveterol has been structurally optimized to show enhanced binding potency compared to its parent monomer .
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guineapig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
GDC-0334 is a selective TRPA1 antagonist. GDC-0334 inhibits TRPA1 function on airway smooth muscle and sensory neurons by decreasing cough and allergic airway inflammation in rats and guineapigs. GDC-0334 can be used for TRPA1-mediated diseases research, such as pain or asthma .
SCH-43478 is a non-nucleoside antiviral agent. SCH-43478 shows potent and selective activity against herpes simplex virus type 2 (HSV-2) with an IC50 of 1.8 μg/mL using Vero cells. SCH-43478 demonstrates significant efficacy in the guineapig genital model of HSV infection .
SC-50605 and SC-51146 are second-generation leukotriene B4 (LTB4) receptor antagonists that effectively inhibit LTB4-induced chemotaxis in guineapigs. SC-50605 targets the LTB4 receptor and has the potential to inhibit inflammatory diseases such as asthma, rheumatoid arthritis, and skin diseases. .
(Rac)-WRC-0571 is a highly potent, orally active and selective, non-xanthine antagonist of A1 adenosine receptors. (Rac)-WRC-0571 inhibits [3H]-N6-cyclohexyladenosine (CHA) binding to guineapig A1-receptors with a Ki value of 1.1 nM .
BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guineapig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7 .
2-Methoxyidazoxan monohydrochloride (RX821002 hydrochloride) is a highly selective alpha 2-adrenoceptor antagonist with little or no imidazoline antagonist effect. RX 821002 has markedly higher affinity for (guinea-pig) alpha 2D-adrenoceptors (pKd 9.7) than for (rabbit) alpha 2A-adrenoceptors (pKd 8.2) .
ROS 234 is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 diaplays poor central access .
L-670596 is an orally active and selective thrombsxane A2 receptor/prostaglandin receptor antagonist. L-670596 inhibits arachidonic acid (HY-109590) and U-44069 induced bronchoconstriction in the guineapig. L-670596 also inhibits the aggregation of human platelet rich plasma induced by U-44069 .
L 743310 is a non-peptide, selective antagonist of the human neurokinin hNK1 receptor, with high affinity for primate and cloned human hNK1 receptors and lower affinity for rodent NK1 receptors. L 743310 inhibits resiniferatoxin-induced plasma protein extravasation in guineapig esophagus. L 743310 has a dose-dependent inhibitory effect on cisplatin-induced emesis .
YM-17690 is a LTD4 and LTE4 agonist, with a pKi value of 9.28 for [3H]LTD4. It induces dose-dependent contractions in guineapig ileum, lung parenchyma, and trachea, with EC50 values of 16, 3.9, and 22 nM, respectively. YM-17690 can be used in research related to asthma and inflammation .
CP-195543 is a potent, selective and orally active leukotriene B4 (LTB4) receptor antagonist with IC50s of 6.8, 37.0 nM for human neutrophils and murine spleen membranes, respectively. CP-195543 blocks CD11b up-regulation. CP-195543 inhibits LTB4-mediated neutrophil infiltration .
β2AR agonist 4 (compound A19) is a potent and selective β2-Adrenoceptor agonist with an EC50 of 3.7 pM. β2AR agonist 4 suppresses the inflammatory cytokines and leukocytes upregulation and improves lung function in COPD rat model .
Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guineapig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively .
Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib sodium exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guineapig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively .
ROS 234 dioxalate is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access .
L-364,373 (R-L3) is a voltage-gated Kv7.1 (KCNQ1)/mink channels activator. L-364,373 activates Iks (slow delayed rectifier potassium current) and shortens action potential duration in guineapig cardiac myocytes, and suppresses early afterdepolarizations in rabbit ventricular myocytes .
NP-1815-PX is a potent and selective P2X4R antagonist. NP-1815-PX has anti-inflammatory activity, and can relieve pain in chronic pain models. NP-1815-PX also inhibits guineapig tracheal/bronchial smooth muscle (TSM and BSM) contractions .
NP-1815-PX sodium is a potent and selective P2X4R antagonist. NP-1815-PX sodium has anti-inflammatory activity, and can relieve pain in chronic pain models. NP-1815-PX sodium also inhibits guineapig tracheal/bronchial smooth muscle (TSM and BSM) contractions .
MIDD0301 (GL-II-93) is an orally effective, anti-asthmatic positive allosteric modulator of GABAA receptor. MIDD0301 had no significant adverse immune reactions at repeated doses and was better than Prednisone (HY-B0214). MIDD0301 relaxes histamine contractions in guineapig and human tracheal smooth muscle for the study of bronchial systolic diseases .
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guineapig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance .
Anatibant (LF 16-0687; XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant crosses the blood-brain barrier (BBB). Anatibant can be used in research on brain damage diseases .
FR 75513 is a 1,1'-biphenyl-2,6-dicarboxylic acid diester series compound that can inhibit the contraction of the detrusor muscle of guineapig bladder (IC50=3.3 μg/mL). After intravenous injection of FR 75513 into anesthetized rats, it also showed strong inhibitory activity on the detrusor contraction (ID50=0.04 mg/kg).
8-O-Acetylharpagide (Standard) is the analytical standard of 8-O-Acetylharpagide. This product is intended for research and analytical applications. 8-O-Acetylharpagide is an iridoid isolated from Ajuga reptans with antitumoral, antiviral, antibacterial, and anti-inflammatory activities. 8-O-Acetylharpagide also has a biological activity on isolated smooth muscle preparations from guineapig .
LY53857 is a potent antagonist of vasoconstriction and serotonin-mediated 5-HT2 receptors. LY53857 did not reduce mean arterial blood pressure in spontaneously hypertensive rats (SHR) at doses that blocked the depressor response to serotonin and blocked central serotonin receptors. In addition, LY53857 was able to enhance neurotransmitter release in rat vas deferens and guineapig ileal nerves .
Anatibant (LF 16-0687; XY-2405) hydrochloride is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant hydrochloride binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant hydrochloride crosses the blood-brain barrier (BBB). Anatibant hydrochloride can be used in research on brain damage diseases .
Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guineapig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guineapig ileum membranes and CHO cells expressing human B1 receptor, respectively.
Asimadoline (EMD-61753) hydrochloride is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guineapig) and 1.2 nM (human recombinant). Asimadoline hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
(-)-Eseroline fumarate is a metabolic of Physostigmine (HY-N6608), an AChE inhibitor. (-)-Eseroline fumarate elicits a leakage of lactic acid dehydrogenase (LDH) from cancer cells. (-)-Eseroline fumarate also induces the release of adenine nucleotides and 5-hydroxytryptamine (5-HT) from neuronal cells, thus induce cell death. (-)-Eseroline fumarate inhibits the electrically evoked twitches of the mouse vas deferens and of the guinea-pig ileum .
5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice .
Clobutinol hydrochloride is a compound that has anti-tussive effects. Clobutinol hydrochloride affects heart rate and blood pressure, it can be used for cough related research .
SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively .
UCB-35440 is an orally active histamine H1 receptor antagonist and 5-lipoxygenase inhibitor. UCB-35440 inhibits LTB4 formation in human whole blood and reduces polymorphonuclear cell infiltration in mouse models. UCB-35440 inhibits histamine-stimulated bronchoconstriction and reduces skin inflammation in guineapigs. UCB-35440 can be used for research on asthma and skin inflammation .
Devazepide (Standard) is the analytical standard of Devazepide. This product is intended for research and analytical applications. Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guineapig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
YM-16638 is an orally active leukotriene (LT) antagonist. YM-16638 can inhibit the production of LTC4, LTD4, and LTE4 in guineapig trachea, with IC50 values of 0.05 μM, 0.16 μM, and 0.096 μM, respectively. YM-16638 has a dose-dependent inhibitory effect on antigen-induced early and late respiratory responses in allergic sheep .
(rel)-MK 287 ((rel)-L-680573) is a relative configuration of MK 287. MK 287, a tetrahydrofuran analog, potently inhibited [ 3H]C18-PAF binding to human platelet, polymorphonuclear leukocyte (PMN) and lung membranes with Kis of 6.1 nM, 3.2 nM and 5.49 nM, respectively. MK 287 inhibits PAF-induced lethality in mice and PAF-induced bronchoconstriction in guineapigs .
Alosetron (GR 68755) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
(5S,6R)-DiHETE is an enantiomer of (5,6)-DiHETEs. (5S,6R)-DiHETE can be recognized by leukotriene receptors (LTD4 receptors). (5S,6R)-DiHETE can induce guineapig isolated ileum contraction? with an EC50 of 1.3 μM, and this effect can be inhibited by LTD4 receptor antagonists .
Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
cis-9,10-Methyleneoctadecanoic acid is a cyclopropane fatty acid that has been found in bacteria and in the digestive glands of P. globosa. It is a component of the cell membrane of Staphylococcus aureus, and levels were reduced after treatment with carvacrol. cis-9,10-Methyleneoctadecanoic acid is secreted by H. pylori and enhances histamine- and dibutyryl cAMP-stimulated acid secretion in isolated guineapig parietal cells. It also activates protein kinase C (PKC) in a calcium-dependent manner.
MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guineapig and human lung membranes, respectively. MK-571 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
BW A575C is a dual inhibitor against angiotensin converting enzyme (ACE) and β-adrenoceptor. BW A575C produces a competitive blockade of Isoprenaline (HY-108353)-induced tachycardia in a guinea-pig right atrial. BW A575C also inhibits Angiotensin I (HY-P1032)-induced pressor responses in rats. BW A575C is promising for research of hypertensive diseases .
Impentamine dihydrobromide (VUF 4702 dihydrobromide) is a histamine H3 receptor antagonist with potential antihistamine activity. Impentamine dihydrobromide shows the strongest selective H3 antagonism among a series of 4(5)-(ω-aminoalkyl)-1H-imidazole compounds. The pA2 value of impentamine dihydrobromide is 8.4, showing its high efficacy in guineapig jejunum. Impentamine dihydrobromide has a specific antagonistic binding site with the H3 receptor .
S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization .
RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guineapig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
SKF-96365 hydrochloride is a potent TRP channel blocker and a store-operated Ca 2+ entry (SOCE) inhibitor. SKF-96365 hydrochloride significantly inhibits hERG, hKCNQ1/hKCNE1, hKir2.1 and hKv4.3 current, and significantly prolongs the QTc interval in isolated guineapig hearts. SKF-96365 hydrochloride exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells .
BW B70C is a potent, selective and orally activearachidonic acid 5-lipoxygenase inhibitor. BW B70C inhibits both acute and allergic bronchoconstriction and late-phase eosinophil accumulation subsequent to allergen inhalation in guinea-pigs. BW B70C prevents leukotriene C4 synthesis and reduces leucocyte migration to the airways lumen as well as albumin microvascular leakage. BW B70C has the potential for the research of anti-asthma agent .
Levobetaxolol is a potent and high affinity β-adrenergic antagonist with IC50 values of 33.2, 2970, 709 nM for guineapig atrial β1, tracheal β2 and rat colonic β3 receptors, respectively. Levobetaxolol reduces IOP (intraocular pressure). Levobetaxolol exhibits a micromolar affinity for L-type Ca21-channels. Levobetaxolol decreases the effects of ischaemia/reperfusion injury in rats. Levobetaxolol has the potential for the research of glaucoma .
(5S,6R)-DiHETEs is the isomer of (5S,6R)-DiHETE (HY-130138A). (5S,6R)-DiHETE can be recognized by leukotriene receptors (LTD4 receptors). (5S,6R)-DiHETE can induce guineapig isolated ileum contraction with an EC50 of 1.3 μM, and this effect can be inhibited by LTD4 receptor antagonists .
RP 72540 is a selective CCK-B receptor antagonist, with IC50 values of 2.4, 1.2, and 3.8 nM for CCK-B receptors in the guineapig cerebral cortex, rat cerebral cortex, and mouse brain, respectively. RP 72540 effectively inhibits CCK-8-induced neuronal firing and dose-dependently inhibits gastric acid secretion, making it potentially valuable in studies of acid secretion. RP 72540 is an important tool for investigating the physiological functions of CCK B receptors .
Ganciclovir triphosphate (GCV-TP) is a synthetic 2'-deoxyguanosine analog with activity in inhibiting human cytomegalovirus (CMV) replication. Ganciclovir triphosphate is effective against CMV infection by binding to viral DNA polymerase and interfering with viral DNA synthesis. Ganciclovir triphosphate has an IC50 of 0.01 μM and has good antiviral effects against CMV strains from humans, monkeys, mice, and guineapigs. Ganciclovir triphosphate has also been used in gene-directed enzyme prodrug inhibition for cancer inhibition .
Parethoxycaine hydrochloride is an anesthetic with nerve conduction blocking activity. Parethoxycaine hydrochloride exhibits non-selective inhibitory effects on responses to various stimulants in rat vas deferens and guineapig ileum muscles. Parethoxycaine hydrochloride has an enhanced effect on the action of norepinephrine, and its methyl bromide derivative also exhibits the same properties on the action of norepinephrine and potassium ions. Derivatives of parethoxycaine hydrochloride have significant effects on calcium dose-response curves, displaying different tissue and stimulant selectivities. The mechanism of action of Parethoxycaine hydrochloride involves the regulation of calcium transport processes .
Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy .
Docosahexaenoyl glycine is a PUFA analogue. Docosahexaenoyl glycine has activating effects on IKs?channels?and restore the function of IKs?channels with LQT1 mutation .
Labetalol (Standard) is the analytical standard of Labetalol. This product is intended for research and analytical applications. Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy .
MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guineapig and human lung membranes, respectively. MK-571 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release .
AZD3839 free base is a potent and selective orally active, brain-permeable BACE1 inhibitor (Ki=26 nM). AZD3839 free base shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 free base exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guineapig, and non-human primate. AZD3839 free base can be used for the research of Alzheimer's disease .
Alosetron (Hydrochloride) (Standard) is the analytical standard of Alosetron (Hydrochloride). This product is intended for research and analytical applications. Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
RG-7152 is a tetrazolyl-substituted leukotriene D4 receptor antagonist that can induce peroxisomal β-oxidation and peroxisome bifunctional enzymes (PBEs) in hepatocytes in various animal models. It has been shown to significantly increase PBE levels and β-oxidation activity in rat and mouse liver homogenates, while smaller effects were observed in guineapigs and monkeys and no effect in dogs. In vitro studies have also shown that it can induce PBEs comparable to clofibric acid, indicating its potential as a peroxisome proliferator .
ZD6021 is an orally active Neurokinin 1 Receptor antagonist, with Ki values of 0.12 nM for NK1 and 0.62 nM for NK2. At a concentration of 100 nM, ZD6021 has a pKB value of 8.9 for human pulmonary artery NK1 receptors, and a pKB value of 7.3 for human bronchial NK2 receptors. ZD6021 effectively reduces ASMSP-induced plasma protein extravasation in guineapigs, with an ED50 of 0.5 mg/kg, and also decreases NK2 mediated bronchoconstriction, with an ED50 of 13 mg/kg .
Moveltipril calcium (MC-838 calcium) is an orally active angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Moveltipril calcium binds via a stable thioester bond and exhibits relative resistance to enzymatic hydrolysis in rat liver homogenate. Moveltipril calcium effectively inhibits ACE extracted from rabbit lung in a concentration-dependent manner. Moveltipril calcium is able to highly specifically inhibit the contractile response to angiotensin-I (AI) in free rat aortic rings and guineapig ileum preparations, while enhancing the contractile response to calcitonin .
Manidipine dihydrochloride is a third-generation, lipophilic, orally active and highly vasoselective calcium channel antagonist (IC50 = 2.6 nM in guinea-pig ventricular cells) and acts as an antihypertensive agent. Manidipine effectively reduces blood pressure as well as improving insulin sensitivity, renal protection, and antiatherosclerotic activity. Manidipine also exerts anti-inflammatory activity mediated by NF-κB and antiviral activity against many flavivirus and negative-strand RNA viruses through the inhibition of calcium channel. Manidipine is widely applied to research of cardiovascular, metabolic disease and infection .
Pentoxyverine (Standard) is the analytical standard of Pentoxyverine. This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membran σ1, respectively. Pentoxyverine is a muscarinic antagonist. Pentoxyverine is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance .
BTM-1042 is a newly synthesized compound with antispasmodic effects. It can inhibit the twitch reaction of the guineapig ileum under electrical stimulation and is not affected by naloxone. It has similar effects to atropine and can block muscarinic receptors, but has less effect on other types of receptors. BTM-1042 also has an inhibitory effect on the ileal reaction caused by nicotine and 5-hydroxytryptamine. BTM-1042 showed a dose-dependent inhibitory effect on the spontaneous movement of the rabbit stomach. In general, BTM-1042 is a agent with a strong antispasmodic effect.
(-)-Pimobedan is an isomer of pimobedan. It has the property of stereoselective partitioning or distribution into erythrocytes. The clearance of (-)-pimobedan from erythrocytes is significantly lower than that of (+)-pimobedan, which is entirely due to its stereoselective distribution into erythrocytes. This stereoselective property of (-)-pimobedan may explain the phenomenon previously reported that it produces a 1.5-fold greater contractile force than the (+)-isomer in detergent-treated myocardial specimens of guineapigs and dogs. These properties suggest that (-)-pimobedan may have unique advantages in terms of in vivo distribution and pharmacological action, which may have important implications for its clinical use.
Alosetron (GR 68755) Hydrochloride(1:X) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride(1:X) is used for the research of irritable bowel syndrome (IBS). Alosetron Hydrochloride(1:X) blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride(1:X) attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
Alosetron (GR 68755) (Z)-2-butenedioate is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron (Z)-2-butenedioate is used for the research of irritable bowel syndrome (IBS). Alosetron (Z)-2-butenedioate blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron (Z)-2-butenedioate attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
ICA-069673 is a KCNQ2/Q3potassium channel activator. ICA-069673 demonstrates greater selectivity for KV7.2/7.3 over KV7.3/KV7.5, with EC50s of 0.69 μM and 14.3 μM, respectively. ICA-069673 inhibits spontaneous phasic and nerve-evoked contractions in guineapig detrusor smooth muscle (DSM). ICA-069673 also decreases the global intracellular Ca(2+) concentration in DSM cells .
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guineapig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .
Pentoxyverine (citrate) (Standard) is the analytical standard of Pentoxyverine (citrate). This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance [4].
Thiosemicarbazide is a vitamin B6 antagonist with anti-acne activity. Thiosemicarbazide is also a well-known source in the synthesis of heterocycles, and its derivatives have potential anticancer activity. Thiosemicarbazide (TSC: HL1) reacts with metal salts, urea (U), to prepare Co(II) and Cu(I) metal complexes. Thiosemicarbazide is also used in the fields of media communications and optical storage, and in the spectrophotometric detection of metals .
PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guineapig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity .
PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guineapig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity .
Toladryl is a derivative of Diphenhydramine (HY-B0303), capable of penetrating the blood-brain barrier and possessing oral activity, as well as antihistamine and anticholinergic activities. The anticholinergic activity of Toladryl is approximately one-tenth that of Diphenhydramine (HY-B0303), and its protective effect against lethal doses of histamine in guineapigs is 2 to 4 times that of Diphenhydramine (HY-B0303). The side effects of Toladryl are fewer and milder than those of Diphenhydramine (HY-B0303), but at higher doses, it may cause central nervous system symptoms such as insomnia, agitation, and disorientation. Toladryl can be used for research in allergic diseases .
RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guineapig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
LY 171859 is a D2 receptor agonist with significant reductase activity. LY 171859 exhibits enzymatic activity in the cytoplasm of liver, lung, and kidney, and also contains significant reductase activity in rat and human blood. LY 171859 has higher hepatic reductase activity in guineapigs, followed by hamsters, rabbits, rats, and mice. The substrate of LY 171859 shows an apparent Km of 5.6 μM. The reduction reaction of LY 171859 is NADPH-dependent with an apparent Km of 14.8 μM. Only the A-side hydrogen of NADPH is incorporated in the reduction product of LY 171859. The reaction of LY 171859 is inhibited by cyanide and thiol reagents, and phenobarbital does not induce its activity in rats .
RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research .
Toladryl (Standard) is the analytical standard of Toladryl. This product is intended for research and analytical applications. Toladryl is a derivative of Diphenhydramine (HY-B0303), capable of penetrating the blood-brain barrier and possessing oral activity, as well as antihistamine and anticholinergic activities. The anticholinergic activity of Toladryl is approximately one-tenth that of Diphenhydramine (HY-B0303), and its protective effect against lethal doses of histamine in guineapigs is 2 to 4 times that of Diphenhydramine (HY-B0303). The side effects of Toladryl are fewer and milder than those of Diphenhydramine (HY-B0303), but at higher doses, it may cause central nervous system symptoms such as insomnia, agitation, and disorientation. Toladryl can be used for research in allergic diseases .
Vapitadine hydrochloride (Compound 3a) is a selective, orally active and nonsedating antihistamine agent, which exhibits a good binding affinity with human cloned histamine H1 receptor with a Ki of 19 nM. Vapitadine hydrochloride decreases the histamine-induced lethality (ED50 is 0.056-1.2 mg/kg), antagonizes the cutaneous reactions to histamine (ED50 is 0.51-1.4 mg/kg) in rats .
Aprikalim (RP 52891), a potassium channel opener (KCO), activates ATP-sensitive K+ (KATP) channels in guineapig ventricular myocytes. Using patch-clamp techniques, it was found that aprikalim enhances KATP channel activity more effectively in Mg-NDP solution compared to standard solutions. In Mg-NDP solution, aprikalim reduced the sensitivity of KATP channels to ATP, increasing the concentration of ATP required to inhibit channel activity by half (K1) from 56 μM to 180 μM. However, this effect diminished over time. Aprikalim's ability to activate KATP channels in Mg-NDP solution suggests potential therapeutic implications in modulating cardiac excitability and may relate to changes in channel protein enzymatic activity under experimental conditions .
LND 796 is an aminosteroidal derivative with positive inotropic effects similar to those of digitalis. It exhibits electrophysiological, toxic, and inotropic effects in normal and partially potassium-depolarized ventricular muscles. LND 796 requires higher concentrations than digoxin to induce the same toxic symptoms. It exhibits a concentration-dependent positive inotropic effect on guineapig papillary muscles in normal potassium solution. In partially potassium-depolarized papillary muscles, LND 796 enhances both components of contraction and increases the amplitude of slow action potentials. The mechanism of positive inotropic action of LND 796 involves enhanced calcium entry in calcium channels and inhibition of sodium-potassium ATPase. Due to its expanded positive inotropic range, LND 796 may have potential application in the treatment of congestive heart failure.
CS-003 is a triple neurokinin receptor antagonist with activity in inhibiting neurokinin-related respiratory diseases. CS-003 exhibits high affinity for human neurokinin 1, 2 and 3 receptors, withKi values of 2.3 nM, 0.54 nM and 0.74 nM respectively. The Ki values of CS-003 on the guineapig neurokinin receptor are 5.2 nM, 0.47 nM and 0.71 nM respectively, showing superior inhibitory effect. CS-003 significantly inhibits the formation of inositol phosphate involving substance P, neurokinin A and neurokinin B through competitive antagonism. CS-003 significantly inhibits citric acid-induced cough, and its effect is better than other selective neurokinin receptor antagonists .
2-Chloro-ATP sodium (2-Chloro ATP) is an adenine nucleotide and an analog of ATP. It is an antagonist of the purinergic P2Y1 receptor and inhibits intracellular calcium mobilization induced by ADP (HY-W010918) in Jurkat cells expressing the human receptor (Ki=2.3 μM). 2-Chloro-ATP sodium is an agonist of the purinergic P2X receptor and induces inward currents in HEK293 cells expressing human bladder smooth muscle or rat PC12 forms of the receptor (EC50=0.5 and 2.5 μM). 2-Chloro-ATP sodium induces relaxation of precontracted guineapig cecal strips in a concentration-dependent manner. 2-Chloro-ATP sodium has been used to study the substrate specificity of cyclic nucleotide-dependent protein kinases such as protein kinase A (PKA) and PKG.
T-0632 is a CCK A receptor antagonist that exhibits significant pharmacological properties in in vitro studies. T-0632 competitively inhibits the binding of [125I]CCK-8 to rat pancreatic CCK A receptors with a K_i value of 0.24 nM, which is significantly lower than the K_i value for guineapig CCK B receptors. T-0632 has higher selectivity in inhibiting CCK-8-stimulated pancreatic enzyme release, with an IC_50 value of 5.0 nM, which is more advantageous than L-364,718 and loxiglumide. In rabbit gallbladder smooth muscle, the antagonistic effects of T-0632 and loxiglumide are reversible, while L-364,718 shows a persistent inhibitory effect. These results indicate that T-0632 is a highly potent, reversible and more selective CCK A receptor antagonist.
(R,R)-MK 287 is a tetrahydrofuran derivative that effectively inhibits the binding of [3H]C18-PAF to human platelets, polymorphonuclear leukocytes (PMNs), and lung membranes with K1 values of 6.1 ± 1.5, 3.2 ± 0.7, and 5.49 ± 2.3 nM, respectively. The inhibition is stereospecific and competitive. Its racemate, L-668,750, is less potent, and its enantiomer, L-680574, is only 1/20 as potent as MK 287. MK 287 inhibits the binding of [3H]C18-PAF to human PMN membranes, reducing the affinity of the radioligand without changing the number of receptor sites. The binding of other radioligands (e.g., LTB4, LTC4, C5a, FMLP) to their specific receptors is unchanged at 1-10 microM MK 287. [3H]MK 287 binds to human platelet and PMN membranes with KD values of 2.1 ± 0.6 and 2.9 ± 1.2 nM. When tested on isolated human cells, MK 287 potently and selectively inhibits PAF-induced platelet aggregation (ED50 = 56 ± 38 nM or ED50 = 1.5 ± 0.5 nM for gel-filtered platelets) and elastase release from PMNs (ED50 = 4.4 ± 2.6 nM). In vivo studies, MK 287 inhibited PAF-induced lethality in mice (ED50 = 0.8 mg/kg oral) and PAF-induced bronchospasm in guineapigs (ED50 = 0.18 mg/kg intraduodenally and 0.19 mg/kg intravenously). The inhibition of PAF-induced bronchospasm was accompanied by a rightward shift in the concentration-response curve for PAF-induced platelet aggregation measured in vitro.
Quinophthalone is a dye with distinctive greenish yellow color. Quinophthalone is used as coloring agents for various materials. Quinophthalone is a strong sensitizer in guineapigs, and its threshold concentration for induction and challenge is 10 ppm .
cis-9,10-Methyleneoctadecanoic acid is a cyclopropane fatty acid that has been found in bacteria and in the digestive glands of P. globosa. It is a component of the cell membrane of Staphylococcus aureus, and levels were reduced after treatment with carvacrol. cis-9,10-Methyleneoctadecanoic acid is secreted by H. pylori and enhances histamine- and dibutyryl cAMP-stimulated acid secretion in isolated guineapig parietal cells. It also activates protein kinase C (PKC) in a calcium-dependent manner.
VIP Guineapig (Vasoactive intestinal peptide), a trophic and mitogenic factor, stimulates growth in whole cultured embryos. VIP Guineapig functions as a simple gastrointestinal hormone and suggest a possible neurotransmitter function .
VIP Guineapig TFA (Vasoactive intestinal peptide), a trophic and mitogenic factor, stimulates growth in whole cultured embryos. VIP Guineapig functions as a simple gastrointestinal hormone and suggest a possible neurotransmitter function .
Scyliorhinin I is a tachykinin-1 (NK-1) and tachykinin-2 (NK-2) receptor agonist with a Ki value of 0.9 nM for rat submandibular gland NK-1 receptor and 2 nM for hamster bladder NK-2 receptor. Scyliorhinin I has the ability to contract the longitudinal muscles of the guineapig ileum .
Des-[Gly77,His78] Myelin Basic Protein (68-84) is a 68-84 sequence fragment of guineapig myelin basic protein (GPMBP). Des-[Gly77,His78] Myelin Basic Protein (68-84) regulates functionally diverse encephalitogenic and proliferative activities of experimental autoimmune encephalomyelitis (EAE)-associated T cells .
Berlopentin (Diacetylsplenopentine) is an antiviral agent, and protects guineapigs from foot-and-mouth disease (FMD) infection. Berlopentin has immunostimulatory properties .
Leumorphin, human is a potent kappa opioid receptor (κ opioid receptor) agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guineapig ileum .
QWF Peptide (Compound 4a) is a substance P antagonist with an IC50 of 0.09 μM. QWF Peptide antagonizes the SP-induced contraction of isolated guineapig trachea strips with an IC50 of 4.7 μM .
[Pro34]Neuropeptide Y, porcine is a selective NPY receptor (Y1 receptor) agonist. [Pro34]Neuropeptide Y, porcine evokes vasoconstrictions in the guineapig caval vein .
PL-3994 is a natriuretic peptide receptor-A (NPR-A) agonist that is resistant to neutral endopeptidase and acts as a bronchodilator. PL-3994 produces concentration-dependent relaxation of pre-contracted guinea-pig trachea with an IC50 value of 42.7 nM .
Peptide M is a synthetic amino acid (18 amino acids in length which correspond to the amino acid positions 303-322 of bovine S-antigen: DTNLASSTIIKEGIDKTV), is capable of inducing experimental autoimmune uveitis in monkeys and Hartley guineapigs as well as Lewis rats .
Substance P (2-11) is a substance P (SP) fragment peptide. Substance P (2-11) has contracting activities on guineapig ileum. Substance P (2-11) inhibits the permeation of 3H SP in BBMEC monolayers .
Substance P (3-11) is a substance P (SP) fragment peptide that can cross the BBB. Substance P (3-11) has contracting activities on guineapig ileum. Substance P (3-11) also promotes human monocyte chemotaxis .
A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guineapig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively .
[D-Trp11]-Neurotensin, an analogue of Neurotensin (NT), is a selective antagonist of NT in perfused rat hearts but behaves as a full agonist in guineapig atria and rat stomach strips. [D-Trp11]-Neurotensin can inhibit NT-induced hypotension .
JMV 449 is a potent neurotensin receptor agonist. JMV 449 shows an IC50 of 0.15 nM for inhibition of [ 125I]-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 has highly potent and long-lasting hypothermic and analgesic effects in the mouse .
JMV 449 acetate is a potent neurotensin receptor agonist. JMV 449 acetate shows an IC50 of 0.15 nM for inhibition of 125I-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 acetate has highly potent and long-lasting hypothermic and analgesic effects in the mouse .
Docosahexaenoyl glycine is a PUFA analogue. Docosahexaenoyl glycine has activating effects on IKs?channels?and restore the function of IKs?channels with LQT1 mutation .
[D-Pro2,D-Phe7,D-Trp9] Substance P is a Substance P (HY-P0201) analogue. [D-Pro2,D-Phe7,D-Trp9] Substance P is an inhibitor of Substance P. [D-Pro2,D-Phe7,D-Trp9] Substance P contracts guinea-pig ileum (GPI) indirectly .
Tyr-α-CGRP (human) TFA is an N-terminally extended human α-CGRP analog. Tyr-α-CGRP (human) TFA can bind to membrane preparations from rat brain and spleen with IC50 values of 0.2 nM and 0.5 nM, respectively, and induce positive chronotropic and inotropic effects in isolated guineapig right and left atria with EC50 values of 282 nM and 74 nM, respectively. Tyr-α-CGRP (human) TFA also inhibits contractile responses in rat vas deferens with an EC50 value of 1.9 nM .
Gigantol is a natural product that could be isolated from Cymbidium giganteum. Gigantol is a potent inhibitor of the spontaneous contractions of the guinea-pig ileum .
3-Methylxanthine, a xanthine derivative, is a cyclic guanosine monophosphate (GMP) inhibitor, with an IC50 of 920 μM on guinea-pig isolated trachealis muscle.
Melitidin is a flavanone glycoside, that can be isolated from Citrus grandis 'Tomentosa'. Melitidin shows a good antitussive effect on cough induced by citric acid in Guineapig .
Nyasicoside is a norlignan glucosides that can be isolated from Curculigo capitulate. Nyasicoside has potent activity against ouabain-induced arrhythmia in the heart preparations of guineapig .
11-trans Leukotriene E4 is an isomer of Leukotriene E4 (LTE4). Slow isomerization of the C-11 double bond of LTE4 leads to the formation of 11-trans LTE4. 11-trans Leukotriene E4 is equipotent to LTE4 in contracting guineapig ileum .
Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with Ki values of 12, 42 and 43 μM at the guineapig, rat and human neurokinin NK1 receptors, respectively .
Onitin is a natural product, that can be isolated from Onychium siliculosum. Onitin is also a non-competitive antagonist of histamine. Onitin shows activity in blocking the peristaltic reflex of the guinea-pig ileum, in inhibition of the responses of guinea-pig ileum to histamine and of inhibition of the responses of guinea-pig tracheal muscle to histamine .
Helveticoside (Strophanthidin-digitoxoside) is a helveticosid, possesses an ED50 of 0.17 μM for isolated guinea-pig ileum. Helveticoside has anticancer effect .
Withanoside V (Standard) is the analytical standard of Withanoside V. This product is intended for research and analytical applications. Withanoside V, a withanolide glycoside, exhibits inhibitory activity for tachyphylaxis to Clonidine in isolated guinea-pig ileum .
8-O-Acetylharpagide is an iridoid isolated from Ajuga reptans with antitumoral, antiviral, antibacterial, and anti-inflammatory activities. 8-O-Acetylharpagide also has a biological activity on isolated smooth muscle preparations from guineapig .
Conessine, a steroidal alkaloid, is a potent and selective histamine H3 receptor antagonist with Kis of 5.4, 6.0, 5.7 and 25 nM for human, dog, guineapig, and rat H H3 receptor, respectively. Anti-malarial activity .
3-Methylxanthine (Standard) is the analytical standard of 3-Methylxanthine. This product is intended for research and analytical applications. 3-Methylxanthine, a xanthine derivative, is a cyclic guanosine monophosphate (GMP) inhibitor, with an IC50 of 920 μM on guinea-pig isolated trachealis muscle.
Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes . Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells .
Gardneramine is an orally active alkaloid that acts like papaverine. Gardneramine has peripheral vascular diastolic effect, direct inhibition on myocardium and central inhibition. Gardneramine showed antihypertensive, vasodilatation and atrial inhibition effects in rabbit, dog and guineapig models, respectively. Gardneramine also inhibits the movement of smooth muscle organs such as the stomach and intestines .
8-O-Acetylharpagide (Standard) is the analytical standard of 8-O-Acetylharpagide. This product is intended for research and analytical applications. 8-O-Acetylharpagide is an iridoid isolated from Ajuga reptans with antitumoral, antiviral, antibacterial, and anti-inflammatory activities. 8-O-Acetylharpagide also has a biological activity on isolated smooth muscle preparations from guineapig .
Docosahexaenoyl glycine is a PUFA analogue. Docosahexaenoyl glycine has activating effects on IKs?channels?and restore the function of IKs?channels with LQT1 mutation .
CTLA-4 protein, a potent inhibitory receptor, plays a crucial role in suppressing T-cell responses by binding strongly to its ligands CD80 and CD86, surpassing the affinity of CD28. This heightened affinity allows CTLA-4 to act as a major negative regulator, maintaining immune homeostasis and preventing excessive T-cell activation. The balance between CTLA-4 and its ligands is pivotal for immune regulation. CTLA-4 Protein, Guinea pig (P.pastoris, His) is the recombinant CTLA-4 protein, expressed by P. pastoris , with C-6*His labeled tag. The total length of CTLA-4 Protein, Guinea pig (P.pastoris, His) is 125 a.a., with molecular weight of ~18.0 kDa.
Azimilide-d8 (dihydrochloride) is the deuterium labeled Azimilide dihydrochloride. Azimilide Dihydrochloride (NE-10064 Dihydrochloride) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
3-Methylxanthine-d3 is deuterated labeled 3-Methylxanthine (HY-50723). 3-Methylxanthine, a xanthine derivative, is a cyclic guanosine monophosphate (GMP) inhibitor, with an IC50 of 920 μM on guinea-pig isolated trachealis muscle.
Rupatadine-d4 (fumarate) is a deuterium labeled Rupatadine fumarate. Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 μM(rabbit platelet membranes/guineapig cerebellum membranes)[1][2][3].
3-Methylxanthine- 13C4, 15N3 is the 13C-labeled and 15N-labeled 3-Methylxanthine. 3-Methylxanthine, a xanthine derivative, is a cyclic guanosine monophosphate (GMP) inhibitor, with an IC50 of 920 μM on guinea-pig isolated trachealis muscle.
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