Search Result
Results for "
less-active
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-15084A
-
(-)-MK-801 maleate
|
iGluR
|
Neurological Disease
|
(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects .
|
-
-
- HY-15652
-
ONO-6818; ONO-PO-736
|
Elastase
|
Inflammation/Immunology
|
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity .
|
-
-
- HY-14864A
-
-
-
- HY-13735C
-
|
Bacterial
|
Infection
|
l-Atabrine dihydrochloride is a less active enantiomer of quinacrine which displays antiprion activity.
|
-
-
- HY-124909
-
-
-
- HY-13079
-
GDC-0973 (R-enantiomer); XL-518 (R-enantiomer)
|
MEK
|
Cancer
|
Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
|
-
-
- HY-100029B
-
|
HBV
|
Infection
|
Bay 41-4109 less active enantiomer shows less activity than Bay 41-4109. BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM.
|
-
-
- HY-126047B
-
|
NF-κB
Amyloid-β
nAChR
|
Neurological Disease
Inflammation/Immunology
|
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist . Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment .
|
-
-
- HY-15652A
-
ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate
|
Elastase
|
Inflammation/Immunology
|
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity .
|
-
-
- HY-14645B
-
rel-DHMEQ
|
NF-κB
|
Cancer
|
DHMEQ racemate is a NF-κB inhibitor. DHMEQ racemate is less active than (-)-DHMEQ.
|
-
-
- HY-17044A
-
IPI-145 R enantiomer; INK1197 R enantiomer
|
PI3K
|
Cancer
|
Duvelisib R enantiomer is a PI3K inhibitor, which is the less active enantiomer of Duvelisib.
|
-
-
- HY-125784A
-
|
5-HT Receptor
|
Neurological Disease
|
(R)-Viloxazine hydrochloride is a less active R-isomer of Viloxazine hydrochloride. Viloxazine hydrochloride is an effective antidepressant agent .
|
-
-
- HY-114673
-
|
Neurokinin Receptor
|
Others
|
Benzomalvin B is the less active analogs of Benzomalvin A. Benzomalvin B is weakly active against substance P .
|
-
-
- HY-120813A
-
-
-
- HY-145009
-
|
STING
|
Others
|
SN-008, a less active SN-011 analog, can be used as a negative control .
|
-
-
- HY-12872B
-
EGF816 (S-enantiomer)
|
EGFR
|
Others
|
Nazartinib S-enantiomer (EGF816 S-enantiomer) is the less active S-enantiomer of Nazartinib. Nazartinib (EGF816) is an EGFR inhibitor.
|
-
-
- HY-100423A
-
KPT-8602 (Z-isomer)
|
CRM1
|
Cancer
|
Eltanexor Z-isomer (KPT-8602 Z-isomer) is the less active isomer of KPT-8602.
|
-
-
- HY-U00008
-
CP 28888-27
|
IFNAR
|
Infection
|
CP-28888 is an interferon inducer, more potent in mice, but is less active in man and devoid of antirhinovirus effects.
|
-
-
- HY-100742B
-
-
-
- HY-N0756A
-
L-(-)-Bornyl acetate
|
Fungal
|
Infection
|
(-)-Bornyl acetate (L-(-)-Bornyl acetate), isolated from hyssop oil, is a less active enantiomer of (+)-Bornyl acetate. (-)-Bornyl acetate possesses antifungal activity .
|
-
-
- HY-18767A
-
-
-
- HY-16901A
-
ND-630 (S enantiomer); GS-0976 (S enantiomer); NDI-010976 (S enantiomer)
|
Acetyl-CoA Carboxylase
|
Others
|
Firsocostat S enantiomer (ND-630 S enantiomer) is the less active S enantiomer of Firsocostat. Firsocostat is an acetyl-CoA carboxylase (ACC) inhibitor.
|
-
-
- HY-14855A
-
(S)-TR 700; (S)-DA 7157
|
Bacterial
Antibiotic
|
Infection
|
(S)-Tedizolid is the S-enantiomer of Tedizolid. Tedizolid is a novel oxazolidinone with activity against Gram-positive pathogens. (S)-Tedizolid is the less active isomer.
|
-
-
- HY-P5592
-
|
Bacterial
|
Infection
|
Temporin B is an antimicrobial peptide against Gram-positive bacteria. Temporin B is less active against Gram-negative bacteria .
|
-
-
- HY-P5592A
-
|
Bacterial
|
Infection
|
Temporin B acetate is an antimicrobial peptide against Gram-positive bacteria. Temporin B acetate is less active against Gram-negative bacteria .
|
-
-
- HY-B2111
-
-
-
- HY-15853A
-
-
-
- HY-40354B
-
|
JAK
|
Inflammation/Immunology
|
(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
|
-
-
- HY-40354D
-
|
JAK
|
Inflammation/Immunology
|
(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
|
-
-
- HY-112218A
-
|
Bcl-2 Family
|
Cancer
|
(R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special Mcl-1 inhibitor with an IC50 of 1.81 nM.
|
-
-
- HY-12279F
-
TGR-1202 R-enantiomer; RP5264 R-enantiomer
|
PI3K
|
Cancer
|
Umbralisib R-enantiomer (TGR-1202 R-enantiomer) is a PI3Kδ inhibitor, which is the less active enantiomer of TGR-1202.
|
-
-
- HY-16950B
-
(E)-Afimoxifene
|
Estrogen Receptor/ERR
|
Cancer
|
(E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
|
-
-
- HY-10502A
-
IND-58359 S enantiomer; (S)-(-)-R-115777
|
Farnesyl Transferase
|
Cancer
|
Tipifarnib S enantiomer is the S-enantiomer of Tipifarnib. Tipifarnib is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM. Tipifarnib S enantiomer is the less active isomer.
|
-
-
- HY-40354C
-
|
JAK
|
Inflammation/Immunology
|
(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
|
-
-
- HY-B0106A
-
UCB 6474
|
Calcium Channel
|
Neurological Disease
|
Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059) .
|
-
-
- HY-112895A
-
|
Androgen Receptor
|
Cancer
|
(R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer .
|
-
-
- HY-101281B
-
|
mAChR
|
Neurological Disease
|
(R)-VU 6008667, the less active (R)-enantiomer to VU 6008667, is devoid of M5 NAM activity (IC50>10 μM) .
|
-
-
- HY-12993B
-
A-60444 (R enantiomer)
|
RSV
|
Infection
|
RSV604 R enantiomer is the R-enantiomer of RSV604. RSV604 is an inhibitor of respiratory syncytial virus (RSV) replication. R-enantiomer is less active against RSV.
|
-
-
- HY-100664
-
-
-
- HY-18715
-
(S)-Ornidazole; Levornidazole
|
Bacterial
Parasite
|
Infection
|
Ornidazole Levo- is the levo-isomer of Ornidazole. Ornidazole is a 5-nitroimidazole derivative with antiprotozoal and antibacterial properties against anaerobic bacteria. Ornidazole Levo- is the less active isomer.
|
-
-
- HY-W074930
-
(S)-GS 1278; (S)-PMPA; (S)-TDF
|
HIV
HBV
|
Infection
|
(S)-Tenofovir ((S)-GS 1278) is the less active S-enantiomer of Tenofovir. Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV) .
|
-
-
- HY-12481A
-
|
PI3K
|
Cancer
|
SAR405 R enantiomer is the less active enantiomer of SAR405. SAR405 is a PIK3C3/Vps34 inhibitor.
|
-
-
- HY-50949A
-
|
IKK
|
Inflammation/Immunology
|
Bay 65-1942 R form is the less active R-form of Bay 65-1942. Bay 65-1942 is an ATP-competitive and selective IKKβ inhibitor.
|
-
-
- HY-12305A
-
(R)-QVD-OPH; (R)-Quinoline-Val-Asp-Difluorophenoxymethylketone
|
Apoptosis
|
Cancer
|
(R)-Q-VD-OPh ((R)-QVD-OPH) is the less active enantiomer of Q-VD-OPha. Q-VD-OPha is an irreversible pan-caspase inhibitor with potent antiapoptotic properties.
|
-
-
- HY-13749C
-
(S)-MK-0431 phosphate
|
Dipeptidyl Peptidase
Autophagy
|
Metabolic Disease
|
(S)-Sitagliptin phosphate is the less active S-enantiomer of Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
|
-
-
- HY-100540C
-
GCA-1
|
Drug Isomer
|
Infection
|
Golgicide A-1 (GCA-1) is a less active cis-diastereomer of Golgicide A (GCA). Golgicide A-1 weakly inhibits mosquito reproduction .
|
-
-
- HY-114277B
-
AMG-510 isomer
|
Ras
|
Others
|
Sotorasib (AMG-510) isomer is the less active isomer of Sotorasib (AMG-510). AMG-510 is a potent KRAS G12C covalent inhibitor.
|
-
-
- HY-19414A
-
-
-
- HY-U00417
-
|
Ras
|
Cancer
|
ARS-1630, a less active enantiomer of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.
|
-
-
- HY-122167
-
-
- HY-122808
-
|
mGluR
|
Metabolic Disease
|
(-)-Camphoric acid is the less active enantiomer of Camphoric acid. Camphoric acid stimulates osteoblast differentiation and induces glutamate receptor expression. Camphoric acid also significantly induced the activation of NF-κB and AP-1 .
|
-
- HY-W067479
-
|
Insecticide
|
Others
|
(E)-Cinnamamide, the less active isomer of Cinnamamide. Cinnamamide, a derivative of the plant secondary compound Cinnamic acid. Cinnamamide is effective as a non-lethal chemical repellent suitable for reducing avian pest damage .
|
-
- HY-B1259
-
Acexamic Acid; 6-Acetamidocaproic acid
|
Drug Metabolite
|
Others
|
6-Acetamidohexanoic acid is a metabolite of hexamethylene bisacetamide (HY-124284). 6-Acetamidohexanoic acid is less active than the parent compound HMBA and cannot induce cell differentiation .
|
-
- HY-N0756AR
-
|
Fungal
|
Infection
|
(-)-Bornyl acetate (Standard) is the analytical standard of (-)-Bornyl acetate. This product is intended for research and analytical applications. (-)-Bornyl acetate (L-(-)-Bornyl acetate), isolated from hyssop oil, is a less active enantiomer of (+)-Bornyl acetate. (-)-Bornyl acetate possesses antifungal activity .
|
-
- HY-107777A
-
|
Histone Methyltransferase
|
Cancer
|
LLY-284 is the diastereomer of LLY-283 with much less active. LLY-283 is a potent inhibitor of PRMT5. LLY-284 has the potential for the research of cancer diseases .
|
-
- HY-101140A
-
-
- HY-19908B
-
|
Elastase
|
Metabolic Disease
|
(R)-BAY-85-8501 is the less active Enantiomer of BAY-85-8501. BAY-85-8501 is a selective and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM .
|
-
- HY-134775A
-
|
Polo-like Kinase (PLK)
|
Cancer
|
PLK4-IN-3 is a less active absolute stereochemistry of PLK4-IN-1. PLK4-IN-1 is a PLK4 inhibitor, with an IC50 of 0.65 μM .
|
-
- HY-B0106AS
-
-
- HY-101682B
-
|
Neprilysin
|
Cardiovascular Disease
Others
|
(R)-SCH 42495 is the less active enantiomer of SCH 42495 . SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester proagent of SCH 42354 .
|
-
- HY-U00193
-
|
Na+/K+ ATPase
|
Metabolic Disease
|
Ro18-5362 is the less active proagent of Ro 18-5364. Even at concentrations as high as 0.1 mM Ro 18-5362 fails to affect significantly (H ++K +)-ATPase activity and associated proton translocation.
|
-
- HY-100729A
-
|
Epigenetic Reader Domain
|
Cancer
|
GSK9311 hydrochloride, a less active analogue of GSK6853, can be used as a negative control. GSK9311 hydrochloride inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively .
|
-
- HY-131328A
-
(R)-LOXO-305
|
Btk
|
Others
|
(R)-Pirtobrutinib ((R)-LOXO-305) is a less active enantiomer of Pirtobrutinib. Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations .
|
-
- HY-133016A
-
|
MetAP
|
Others
|
(R)-M8891 (compound R-9) is a less active isomer of M8891. M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor .
|
-
- HY-B0106AR
-
|
Calcium Channel
|
Neurological Disease
|
Etiracetam (Standard) is the analytical standard of Etiracetam. This product is intended for research and analytical applications. Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059) .
|
-
- HY-100729
-
|
Epigenetic Reader Domain
|
Cancer
|
GSK9311, a less active analogue of GSK6853, can be used as a negative control. GSK9311 inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively .
|
-
- HY-141454A
-
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
TLR8 agonist 2 hydrochloride is a potent and selective TLR8 agonist with an EC50 of 3 nM for human TLR8. TLR8 agonist 2 hydrochloride shows less active against human TLR7 (EC50 of 33.33 μM) .
|
-
- HY-141454
-
-
- HY-101533B
-
|
Bcl-2 Family
|
Cancer
|
AZD-5991 S-enantiomer is the less active enantiomer of AZD-5991. AZD-5991 S-enantiomer is a Mcl-1 inhibitor with an IC50 of 6.3 μM in FRET assay and a Kd of 0.98 μM in surface plasmon resonance (SPR) assay.
|
-
- HY-122096
-
DCLX069
1 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects .
|
-
- HY-P2678
-
|
Cholecystokinin Receptor
|
Metabolic Disease
|
CCK (26-31) (non-sulfated) is the N-terminal fragment of CCK, a peptide hormone found in the gut and brain that stimulates digestion, regulates satiety, and is associated with anxiety. CCK (26-31) is also less active in non-sulfated than in sulfated form .
|
-
- HY-18018
-
RN486
3 Publications Verification
|
Btk
|
Inflammation/Immunology
|
RN486 is a potent, selective and orally active Btk inhibitor with an IC50 of 4.0 nM and a Kd of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research .
|
-
- HY-112475
-
|
Tie
FLT3
|
Cancer
|
Flt-3 Inhibitor III is a potent and selective FLT3 kinase inhibitor with an 50 of 50 nM. Flt-3 Inhibitor III shows less active against other kinases. Flt-3 Inhibitor III has anticancer effects .
|
-
- HY-12515B
-
(S)-YC-93 free base
|
Calcium Channel
|
Cardiovascular Disease
Neurological Disease
|
(S)-Nicardipine ((S)-YC-93 free base) is the less active S enantiomer of Nicardipine. Nicardipine is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure .
|
-
- HY-W074930R
-
|
HIV
HBV
|
Infection
|
(S)-Tenofovir (Standard) is the analytical standard of (S)-Tenofovir. This product is intended for research and analytical applications. (S)-Tenofovir ((S)-GS 1278) is the less active S-enantiomer of Tenofovir. Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV) .
|
-
- HY-13749CR
-
|
Dipeptidyl Peptidase
Autophagy
|
Metabolic Disease
|
(S)-Sitagliptin (phosphate) (Standard) is the analytical standard of (S)-Sitagliptin (phosphate). This product is intended for research and analytical applications. (S)-Sitagliptin phosphate is the less active S-enantiomer of Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
|
-
- HY-147829
-
|
Carbonic Anhydrase
|
Cancer
|
hCAXII-IN-2 (compound 5i) is a potent human carbonic anhydrase XII (hCA XII) and hCA IX inhibitor with Ki values of 84.2 nM and 268.5 nM, respectively. hCAXII-IN-2 shows less active against hCA I and hCA II .
|
-
- HY-134753
-
4-Amino-N-(4-trifluoromethylphenyl)benzamide
|
COX
|
Inflammation/Immunology
|
Teriflunomide impurity 3 (4-Amino-N-(4-trifluoromethylphenyl)benzamide) is a selective COX-1 inhibitor with an IC50 of 30 µM. Teriflunomide impurity 3 is less active against COX-2 (IC50>100 µM) .
|
-
- HY-N14932
-
|
Platelet-activating Factor Receptor (PAFR)
|
Cardiovascular Disease
|
Aggreceride A is a platelet aggregation inhibitor. Aggreceride A shows an inhibitory activity against aggregation induced by Adenosine 5'-diphosphate (ADP) (HY-W010918), Arachidonic acid (HY-109590) and PAF (platelet activating factor), but was less active against aggregation induced by collagen .
|
-
- HY-N1778A
-
(E)-O-Methylferulic acid
|
Reactive Oxygen Species
Virus Protease
|
Infection
Cancer
|
(E)-3,4-Dimethoxycinnamic acid is the less active isomer of 3,4-Dimethoxycinnamic acid. 3,4-Dimethoxycinnamic acid exerts anti-apoptotic effects on L-02 cells via the ROS-mediated signaling pathway . Anti-apoptotic effects .
|
-
- HY-123905A
-
|
Drug Isomer
|
Cancer
|
LIN28 inhibitor LI71 enantiomer is the enantiomer of LIN28 inhibitor LI71 with less active. LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM .
|
-
- HY-16723A
-
(R)-TV 45070; (R)-XEN402
|
Sodium Channel
|
Neurological Disease
Inflammation/Immunology
|
(R)-Funapide ((R)-TV 45070) is the less active R-enantiomer of Funapide. Funapide is a potent inhibitor of the sodium channel Nav1.7, Nav1.8 and other Nav channels expressed in the peripheral nervous system. Fornabil is an orally effective analgesic agent .
|
-
- HY-114205A
-
|
Epigenetic Reader Domain
|
Cancer
|
TP-238 hydrochloride is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 hydrochloride also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases .
|
-
- HY-12515C
-
(R)-YC-93 free base
|
Calcium Channel
|
Cardiovascular Disease
Neurological Disease
|
(R)-Nicardipine ((R)-YC-93 free base) is the less active R enantiomer of Nicardipine. Nicardipine (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure .
|
-
- HY-N0136B
-
(-)-Dihydroquercetin
|
Tyrosinase
|
Inflammation/Immunology
|
(-)-Taxifolin is the less active enantiomer of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
|
-
- HY-114205
-
|
Epigenetic Reader Domain
|
Cancer
|
TP-238 is a potent and selective dual CECR2/BPTF probe with IC50 values of 30 nM and 350 nM, respectively. TP-238 also inhibits BRD9 with a pIC50 of 5.9 and is less active against other 338 kinases .
|
-
- HY-115688A
-
|
Arrestin
|
Cardiovascular Disease
Others
|
(S)-TXNIP-IN-1 is the less active S-enantiomer of TXNIP-IN-1 (HY-115688). TXNIP-IN-1 is a TXNIP-TRX complex inhibitor which can be used in the research of TXNIP-TRX complex associated metabolic disorder (diabetes), cardiovascular disease, or inflammatory disease
|
-
- HY-N14933
-
|
Platelet-activating Factor Receptor (PAFR)
|
Cardiovascular Disease
|
Aggreceride B is a platelet aggregation inhibitor. Aggreceride B shows an inhibitory activity against aggregation induced by Adenosine 5'-diphosphate (ADP) (HY-W010918), Arachidonic acid (HY-109590) and PAF (platelet activating factor), but was less active against aggregation induced by collagen .
|
-
- HY-100013B1
-
|
GPR88
Drug Isomer
|
Neurological Disease
|
(1S,2S)-2-PCCA hydrochloride is a less active diastereomer of 2-PCCA. 2-PCCA is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.
|
-
- HY-101093B
-
|
PD-1/PD-L1
|
Cancer
|
PD-1-IN-20 is the less active enantiomer of PD-1-IN-1. PD-1-IN-1 is an inhibitor of programmed cell dealth-1 (PD-1) extracted from patent WO 2015033299 A1, compound example 4 .
|
-
- HY-N14934
-
|
Platelet-activating Factor Receptor (PAFR)
|
Cardiovascular Disease
|
Aggreceride C is a platelet aggregation inhibitor. Aggreceride C shows an inhibitory activity against aggregation induced by Adenosine 5'-diphosphate (ADP) (HY-W010918), Arachidonic acid (HY-109590) and PAF (platelet activating factor), but was less active against aggregation induced by collagen .
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- HY-111532B
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ClpP
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Infection
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(3S,4S)-A2-32-01 (compound 24(S,S)), a less active (S,S)-enantiomer of A2-32-01. A2-32-01 is a potent caseinolytic protein proteases (ClpP) inhibitor .
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- HY-16950BS
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(E)-Afimoxifene-d5
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Isotope-Labeled Compounds
Estrogen Receptor/ERR
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Cancer
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(E)-4-Hydroxytamoxifen-d5 ((E)-Afimoxifene-d5) is the deuterium labeled (E)-4-Hydroxytamoxifen. (E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
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- HY-107597
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Halicin
1 Publications Verification
SU3327
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JNK
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Metabolic Disease
Inflammation/Immunology
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Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt kinase .
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- HY-A0295
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- HY-130696
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(+)-Trans-(1R,2R)-U-50488
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Opioid Receptor
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Neurological Disease
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(+)-U-50488 ((+)-Trans-(1R,2R)-U-50488) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .
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- HY-15997A
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(+)-Trans-(1R,2R)-U-50488 hydrochloride
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Opioid Receptor
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Neurological Disease
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(+)-U-50488 (hydrochloride) (+)-Trans-(1R,2R)-U-50488 hydrochloride) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .
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- HY-10791
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- HY-43913
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Eukaryotic Initiation Factor (eIF)
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Others
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(R)-eIF4A3-IN-2 is a less active enantiomer of eIF4A3-IN-2. eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 (eIF4A3) inhibitor with an IC50 of 110 nM .
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- HY-112346
-
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CDK
Apoptosis
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Cancer
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RGB-286147 is a selective and ATP-competitive CDK and CDK-related kinases (CRK) inhibitor with IC50 values ranging from 9-839 nM. RGB-286147 shows less active against other non-CDK/CRK kinases. RGB-286147 induces cell apoptosis, and exhibits anti-tumor activity .
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- HY-13728A
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(R)-ZD 9331; (R)-BGC9331
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Biochemical Assay Reagents
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Cancer
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(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed . Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor . (R)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-108235C
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(R)-AZD6765
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iGluR
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Neurological Disease
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(R)-Lanicemine ((R)-AZD6765) is the less active R-enantiomer of Lanicemine. Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively). Antidepressant effects .
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- HY-100740C
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(1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814
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Beta-secretase
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Neurological Disease
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(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat. Lanabecestat is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM .
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- HY-108425A
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Sodium Channel
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Neurological Disease
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AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC50s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM .
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- HY-12885C
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ADU-S100 enantiomer ammonium salt; MIW815 enantiomer ammonium salt; ML RR-S2 CDA enantiomer ammonium salt
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IFNAR
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Inflammation/Immunology
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2’3’-c-di-AM(PS)2 (Rp,Rp) enantiomer ammonium salt (ADU-S100 enantiomer ammonium salt) is the less active enantiomer of 2’3’-c-di-AM(PS)2 (Rp,Rp). 2’3’-c-di-AM(PS)2 (Rp,Rp) is an activator of stimulator of interferon genes (STING) .
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- HY-119530
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BW 57-323
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Nucleoside Antimetabolite/Analog
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Others
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Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
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- HY-120982
-
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Prostaglandin Receptor
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Endocrinology
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Cloprostenol is a synthetic prostaglandin F2α (PGF2α) analog and a potent FP receptor agonist. (+)-15-epi Cloprostenol is the 15(S), or 15β-hydroxy enantiomer of (+)-cloprostenol. This epimer is less active by several orders of magnitude as an FP receptor ligand when compared to 15(R)-cloprostenol. However, the specific activity of this isomer has not been well studied.
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- HY-109015
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Tucidinostat
Maximum Cited Publications
24 Publications Verification
Chidamide; HBI-8000; CS 055
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HDAC
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Cancer
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Tucidinostat (Chidamide) is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9 .
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- HY-100764
-
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Histone Demethylase
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Cancer
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YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity .
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- HY-107429
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PF-04965842
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JAK
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Inflammation/Immunology
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Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease .
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- HY-116830A
-
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GSK-3
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Cancer
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(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) .
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- HY-19985A
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EGFR
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Cancer
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(3S, 4S)-PF-06459988 is the S enantiomer of PF-06459988 with less active. PF-06459988 is a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR). PF-06459988 has excellent selectivity against EGFR wild-type while possessing a minimally reactive electrophile that reduces the propensity of off-target labeling .
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- HY-18679
-
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mGluR
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Neurological Disease
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TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo .
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- HY-131312A
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LY3410738 (gentisate); Mutant IDH1-IN-6 (gentisate)
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Isocitrate Dehydrogenase (IDH)
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Cancer
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Crelosidenib (gentisate) is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50 of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Crelosidenib (gentisate) is less active at inhibiting the IDH wild-type enzymes .
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- HY-14202
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Ro 19-6327 hydrochloride
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Monoamine Oxidase
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Neurological Disease
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Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease .
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- HY-14201
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Ro 19-6327
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Monoamine Oxidase
|
Neurological Disease
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Lazabemide (Ro 19-6327) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide ?inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and?alzheimer′s disease .
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- HY-107429R
-
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JAK
|
Inflammation/Immunology
|
Abrocitinib (Standard) is the analytical standard of Abrocitinib. This product is intended for research and analytical applications. Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease .
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- HY-119821R
-
|
Glycosidase
|
Infection
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Thiamiprine (Standard) is the analytical standard of Thiamiprine. This product is intended for research and analytical applications. Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
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- HY-141848A
-
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mGluR
|
Neurological Disease
|
(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC50 >1μM for mGluR5 receptor . BMS-984923 is a potent mGluR5 silent allosteric modulator . (S,S)-BMS-984923 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-119530R
-
|
Nucleoside Antimetabolite/Analog
|
Others
|
Thiamiprine (Standard) is the analytical standard of Thiamiprine. This product is intended for research and analytical applications. Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
|
-
- HY-131312
-
LY3410738; Mutant IDH1-IN-6
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes .
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- HY-100218B
-
|
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
(1R,3S)-RSL3 is the less active (1R,3S)-enantiomer of RSL3 ((1S,3R)-RSL3). (1R,3S)-RSL3 and RSL3 induce cell death in HT22 wild-type cells with EC50 values of 5.2 µM and 0.004 µM, rspectively .
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-
- HY-135976
-
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
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 guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P5592
-
|
Bacterial
|
Infection
|
Temporin B is an antimicrobial peptide against Gram-positive bacteria. Temporin B is less active against Gram-negative bacteria .
|
-
- HY-P5592A
-
|
Bacterial
|
Infection
|
Temporin B acetate is an antimicrobial peptide against Gram-positive bacteria. Temporin B acetate is less active against Gram-negative bacteria .
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-
- HY-P2678
-
|
Cholecystokinin Receptor
|
Metabolic Disease
|
CCK (26-31) (non-sulfated) is the N-terminal fragment of CCK, a peptide hormone found in the gut and brain that stimulates digestion, regulates satiety, and is associated with anxiety. CCK (26-31) is also less active in non-sulfated than in sulfated form .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-16950BS
-
|
(E)-4-Hydroxytamoxifen-d5 ((E)-Afimoxifene-d5) is the deuterium labeled (E)-4-Hydroxytamoxifen. (E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
|
-
-
- HY-B0106AS
-
|
Etiracetam-d3 is the deuterium labeled Etiracetam. Etiracetam (UCB 6474) is an acetylcholine agonist and a nootropic drug of the racetam family. Less active than its S-enantiomer Levetiracetam (UCB L059)[1].
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-13728A
-
(R)-ZD 9331; (R)-BGC9331
|
|
Alkynes
|
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed . Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor . (R)-Plevitrexed is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
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