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kappa-opioid receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Opioid Receptor (73) Adenylate Cyclase (2) Apoptosis (4) Autophagy (2) Caspase (2) CXCR (1) Endogenous Metabolite (2) Ferroptosis (2) iGluR (2) Isotope-Labeled Compounds (2) Mitophagy (2) PINK1/Parkin (2)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Endocrinology (1) Infection (1) Inflammation/Immunology (7) Metabolic Disease (4) Neurological Disease (65)

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nor-Binaltorphimine 4 Publications Verification Norbinaltorphimine; NorBNI	Opioid Receptor	Others
nor-Binaltorphimine is a selective antagonist of **kappa-opioid receptor**. nor-Binaltorphimine has a long-lasting effect in vivo .

Allomatrine (+)-Allomatrine	Others	Neurological Disease
Allomatrine ((+)-Allomatrine) is an alkaloid from the bark of Sophora japonica. Allomatrine has antinociceptive properties mediated mainly through the activation ofκ-opioid receptors .

JDTic dihydrochloride	Opioid Receptor	Neurological Disease
JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.

22-Thiocyanatosalvinorin A RB-64	Opioid Receptor	Neurological Disease
22-Thiocyanatosalvinorin A (RB-64) is a potent and selective **kappa-opioid receptor agonist with an EC₅₀** of 0.077 nM .

BU09059	Opioid Receptor	Neurological Disease
BU09059 is a potent and selective **Kappa-opioid receptor** antagonist with a pA₂ of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception .

Icalcaprant	Opioid Receptor	Neurological Disease
Icalcaprant is a kappa-opioid receptor antagonist .

Enadoline CI-977	Opioid Receptor	Neurological Disease
Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (K_i=1.25 nM). Antinociceptive effects .

Enadoline hydrochloride CI-977 hydrochloride	Opioid Receptor	Neurological Disease
Enadoline (CI-977) hydrochloride is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (K_i=1.25 nM). Antinociceptive effects .

SalA-VS-08	Opioid Receptor	Neurological Disease
SalA-VS-08 is a full agonist of kappa-opioid receptor (KOR) with selectivity and G-protein bias. SalA-VS-08 can be used in the research of analgesia .

SalA-VS-07	Opioid Receptor	Neurological Disease
SalA-VS-07 is a G protein-biased partial agonist for the Kappa-opioid receptor (KOR). SalA-VS-07 can be used for research of pain and other disorders .

5'-Guanidinonaltrindole TFA 5'-GNTI TFA	Others	Neurological Disease
5'-Guanidinonaltrindole TFA is a selective kappa-opioid receptor antagonist with significant opioid antagonist activity. 5'-Guanidinonaltrindole TFA exhibits 5 times the antagonistic potency of the prototypical kappa-opioid receptor antagonist norbinatorphimine in smooth muscle preparations, with a selectivity ratio exceeding 500 times. Binding and functional studies of 5'-Guanidinonaltrindole TFA showed pA(2) values comparable to smooth muscle data. 5'-Guanidinonaltrindole TFA is regarded as a potentially valuable pharmacological tool for studying opioids due to its high selectivity and potency .

5'-Guanidinonaltrindole hydrochloride 5'-GNTI hydrochloride	Opioid Receptor	Neurological Disease
5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent **κ-opioid receptor antagonist with a K_i** of 0.18 nM for human κ-opioid receptor .

Leumorphin, human	Opioid Receptor	Neurological Disease
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 guinea pig ileum .

Riminkefon	Opioid Receptor	Neurological Disease
Riminkefon is a **kappa opioid receptor** agonist .

Norbinaltorphimine dihydrochloride 4 Publications Verification nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride	Opioid Receptor	Neurological Disease
Norbinaltorphimine dihydrochloride is a potent and selective **κ opioid receptor** antagonist.

ML138	Opioid Receptor	Others
ML138, a **κ opioid receptor** agonist, is a MLPCN probe .

Anrikefon HSK21542	Opioid Receptor	Neurological Disease
Anrikefon (HSK21542) is a kappa opioid receptor agonist with analgesic effect .

Anrikefon acetate HSK21542 acetate	Opioid Receptor	Neurological Disease
Anrikefon (HSK21542) acetate is a kappa opioid receptor agonist with analgesic effect .

CR 665 JNJ 38488502; FE 200665	Opioid Receptor	Neurological Disease
CR 665 (JNJ 38488502) is a peripherally selective *κ-opioid* agonist. CR 665 can activate the kappa opioid receptor with EC₅₀ value of 10.9 nM. CR 665 can be used for the research of peripheral pain .

JDTic	Opioid Receptor	Neurological Disease
JDTic is a highly selective antagonist for the κ-opioid receptor; without affecting the μ- or δ-opioid receptors.

DuP 747 hydrochloride	Opioid Receptor	Neurological Disease
DuP 747 hydrochloride is an analgesic with selective kappa-opioid receptor agonist activity. DuP 747 showed less spiradoline-appropriate selection when administered SC, but showed a partial generalized response to spiradoline when administered IP or PO. The 5-hydroxy-desmethoxy metabolite of DuP 747 induced selection of the saline-appropriate lever only. The effects of DuP 747 suggest that its metabolites may play a major role in the similar responses to spiradoline after IP and PO administration .

Porcine dynorphin A(1-13) Dynorphin A Porcine Fragment 1-13	Opioid Receptor	Others
Porcine dynorphin A (1-13) is a potent, endogenous **κ opioid receptor** agonist and is antinociceptive at physiological concentrations.

Aticaprant 5 Publications Verification CERC-501; LY-2456302	Opioid Receptor	Neurological Disease
Aticaprant (CERC-501) is a potent and centrally-penetrant *kappa opioid* receptor antagonist with a K_i of 0.807 nM.

ML 190	Opioid Receptor	Neurological Disease
ML 190 is a selective κ opioid receptor (KOR) antagonist with an IC₅₀ of 120 nM and an EC₅₀ of 129 nM, respectively .

CR 665 acetate JNJ 38488502 acetate; FE 200665 acetate	Others	Neurological Disease
CR 665 (JNJ 38488502) acetate is a kappa-opioid agonist that may effectively treat visceral pain by activating receptors on afferent nerves within the gut. CR 665 acetate exhibits peripheral selectivity, differentiating its pharmacokinetic profile from that of non-selective opioids like oxycodone. CR 665 acetate has demonstrated a beneficial effect on visceral pain tolerance thresholds without the delayed analgesic response characteristic of opioids that penetrate the brain. CR 665 acetate is proposed for use in managing postoperative pain due to its pain-relieving properties.

R-84760	Opioid Receptor	Neurological Disease
R-84760 is a selective **κ-opioid receptor** agonist. R-84760 has antinociceptive effect .

ICI 199441	Opioid Receptor	Cardiovascular Disease
ICI 199441 is a potent and selective *κ-opioid* receptor agonist. ICI 199441 can improve heart resistance to ischemia/reperfusion .

NP-5497-KA	Others	Neurological Disease
NP-5497-KA is a *κ-opioid* receptor agonist. NP-5497-KA has orally activity[1].

U-54494A	Opioid Receptor	Neurological Disease
U-54494A is a benzamide derivative related to κ-opioid *receptor* agonists, U-54494A has an anticonvulsant activity .

MR2034 (R)-UM-1071	Opioid Receptor	Endocrinology
MR2034 ((R)-UM-1071) is a κ-opioid receptor agonist with activity that stimulates the hypothalamic-pituitary-adrenal axis. MR2034 has shown the potential to promote mood and inhibit addictive behaviors in animal models and can be used to study inhibitory approaches related to mood and addictive disorders. MR2034 is selective for κ-opioid receptors and can effectively modulate biological processes related to stress and mood .

Loperamide ADL 2-1294	Opioid Receptor	Inflammation/Immunology
Loperamide (ADL 2-1294) is a selective μ opioid receptor agonist with K_is of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide can be used as an antidiarrheal agent .

DIPPA hydrochloride	Opioid Receptor	Neurological Disease
DIPPA (hydrochloride) is an irreversible, long-lasting, selective and high affinity **κ-opioid receptor** antagonist. DIPPA (hydrochloride) can be used for the research of anxiety and antidepressant .

(±)-U-50488 hydrochloride (±)-Trans-(1R,2R)-U-50488 hydrochloride	Opioid Receptor	Neurological Disease
(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrochloride is a selective κ opioid receptor (KOR) agonist .

(±)-U-50488 hydrate hydrochloride (±)-Trans-(1R,2R)-U-50488 hydrate hydrochloride	Opioid Receptor	Neurological Disease
(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrate hydrochloride is a selective κ opioid receptor (KOR) agonist .

(-)-U-50488 hydrochloride (-)-Trans-(1S,2S)-U-50488 hydrochloride	Opioid Receptor	Infection Cancer
(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (b>K_d=2.2 nM) over *μ-opioid* receptor (MOR) (b>K_d=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+)?trans-(1R,2R) U-50488 (HY-15997A)?or the (±)?trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV** effect in fected blood monocyte-derived macrophages (MDM) .

GR103545	Opioid Receptor	Neurological Disease
GR103545 is a potent and selective agonist of the **κ-opioid receptor (κ-OR)**. ¹¹GR103545 is a radiotracer for imaging κ-OR in vivo ^[1]

Cyprodime hydrochloride	Opioid Receptor	Neurological Disease
Cyprodime hydrochloride is a highly selective μ-opioid receptor antagonist with K_i values of 5.4 nM, 244.6 nM and 2187 nM for μ-, δ- and κ-opioid receptors, respectively. Cyprodime hydrochloride has anti-depressant-like effect .

LY2444296 FP3FBZ	Opioid Receptor	Neurological Disease
LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a K_i value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects .

(1R,2R)-U-50488 hydrochloride	Opioid Receptor	Neurological Disease
(1R,2R)-U-50488 hydrochloride is the absolute stereochemistry of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist .

Dynorphin A (1-10)	Opioid Receptor iGluR	Neurological Disease
Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the **κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC₅₀** of 42.0 μM.

Akuammine (-)-Akuammine; Vincamajoridine	Others	Neurological Disease
Akuammine is an indole alkaloid that has been found in Picralima nitida and has analgesic activity. It selectively binds to the μ- and κ-opioid receptors over the δ-opioid receptor (Kis=0.3, 1.68, and 10.4 μM for the human receptors, respectively). Akuammine inhibits forskolin-induced cAMP production in HEK293 cells expressing human μ- or κ-opioid receptors (IC₅₀s=2.6 and 0.073 μM, respectively). It increases the latency to withdrawal in the tail-flick or hot plate test in mice when administered at a dose of 60 mg/kg.

Dynorphin A (1-10) (TFA)	Opioid Receptor iGluR	Neurological Disease
Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the **κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC₅₀** of 42.0 μM.

UFP-101	Opioid Receptor	Neurological Disease
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pK_i of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect .

*μ/κ/δ opioid* receptor agonist 1**	Opioid Receptor	Inflammation/Immunology
μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .

[DPro10] Dynorphin A (1-11), porcine	Opioid Receptor Adenylate Cyclase	Neurological Disease
[DPro10] Dynorphin A (1-11), porcine, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a K_i value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine has analgesic property .

[DPro10] Dynorphin A (1-11), porcine hydrochloride	Opioid Receptor Adenylate Cyclase	Neurological Disease
[DPro10] Dynorphin A (1-11), porcine hydrochloride, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a K_i value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine hydrochloride has analgesic property .

Cat. No.	Product Name	Target	Research Area

HY-P3609

CR 665 JNJ 38488502; FE 200665	Opioid Receptor	Neurological Disease
CR 665 (JNJ 38488502) is a peripherally selective *κ-opioid* agonist. CR 665 can activate the kappa opioid receptor with EC₅₀ value of 10.9 nM. CR 665 can be used for the research of peripheral pain .

HY-P0088

Porcine dynorphin A(1-13) Dynorphin A Porcine Fragment 1-13	Opioid Receptor	Others
Porcine dynorphin A (1-13) is a potent, endogenous **κ opioid receptor** agonist and is antinociceptive at physiological concentrations.

HY-P1594A

Dynorphin A (1-10) (TFA)	Opioid Receptor iGluR	Neurological Disease
Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds to extracellular loop 2 of the **κ-opioid receptor. Dynorphin A (1-10) (TFA) also blocks NMDA-activated current with an IC₅₀** of 42.0 μM.

HY-P10006

Leumorphin, human	Opioid Receptor	Neurological Disease
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 guinea pig ileum .

HY-P3376

Riminkefon	Opioid Receptor	Neurological Disease
Riminkefon is a **kappa opioid receptor** agonist .

HY-P3445

Anrikefon HSK21542	Opioid Receptor	Neurological Disease
Anrikefon (HSK21542) is a kappa opioid receptor agonist with analgesic effect .

HY-P3445A

Anrikefon acetate HSK21542 acetate	Opioid Receptor	Neurological Disease
Anrikefon (HSK21542) acetate is a kappa opioid receptor agonist with analgesic effect .

HY-P1594

Dynorphin A (1-10)	Opioid Receptor iGluR	Neurological Disease
Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the **κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC₅₀** of 42.0 μM.

HY-P1299

UFP-101	Opioid Receptor	Neurological Disease
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pK_i of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect .

HY-P10203

*μ/κ/δ opioid* receptor agonist 1**	Opioid Receptor	Inflammation/Immunology
μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .

HY-P3647

[DPro10] Dynorphin A (1-11), porcine	Opioid Receptor Adenylate Cyclase	Neurological Disease
[DPro10] Dynorphin A (1-11), porcine, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a K_i value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine has analgesic property .

HY-P3647A

[DPro10] Dynorphin A (1-11), porcine hydrochloride	Opioid Receptor Adenylate Cyclase	Neurological Disease
[DPro10] Dynorphin A (1-11), porcine hydrochloride, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a K_i value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine hydrochloride has analgesic property .

HY-17609

Difelikefalin CR-845; FE-202845	Opioid Receptor	Neurological Disease
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .

HY-P5907

Helianorphin-19	Opioid Receptor	Neurological Disease
Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a K_i of 21 nM and an EC₅₀ of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain .

HY-P1333

Dynorphin A	Opioid Receptor Apoptosis Caspase Endogenous Metabolite	Neurological Disease
Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .

HY-P1299A

UFP-101 TFA	Opioid Receptor	Neurological Disease
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pK_i of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .

HY-P3634

[DAla2] Dynorphin A (1-13), amide (porcine)	Opioid Receptor	Neurological Disease
[DAla2] Dynorphin A (1-13), amide (porcine) is a petide. [DAla2] Dynorphin A (1-13), amide (porcine) might have the κ opioid receptor agonist effect. [DAla2] Dynorphin A (1-13), amide (porcine) can be used for the research of nervous system .

HY-P1333A

Dynorphin A TFA	Opioid Receptor Apoptosis Caspase Endogenous Metabolite	Neurological Disease
Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease .

HY-P4679

(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) E2078	Opioid Receptor	Neurological Disease
(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) (E-2078), a stable Dynorphin A (1–8) (HY-P2159) analog, is a kappa opioid receptor (KOR) agonist .

HY-W019787

BAM-12P	Opioid Receptor CXCR	Neurological Disease
BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate *human κ-opioid* receptor (hKOR) with an EC₅₀ of 101 nM and a pEC₅₀ of 6.99. BAM-12P is a ligand for CXCR7 with an EC₅₀** of 175 nM .

HY-P5892

β-Endorphin (1-27) (human)	Opioid Receptor	Neurological Disease
β-Endorphin (1-27) (human) is an *opioid* antagonist that binds μ-, δ-, and κ-opioid receptors with K_is of 5.31, 6.17, and 39.82 nM, respectively. β-Endorphin (1-27) (human) inhibits β-Endorphin (HY-P1502)-induced and etorphine-induced analgesia .

Cat. No.	Product Name	Chemical Structure

HY-123689S

Samidorphan-d4

Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .

HY-123689S1

Samidorphan-d5

Samidorphan-d5 (ALKS-33-d5) is a tritiated version of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo .

Cat. No.	Compare	Product Name	Application	Reactivity

HY-P83387

	kappa Opioid Receptor Antibody (YA3132) KOR; R21; KOR-1; MSL-1; Oprk2; K-OR-1	WB, IP	Rat
	kappa Opioid Receptor Antibody (YA3132) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA3132), targeting kappa Opioid Receptor, with a predicted molecular weight of 43 kDa (observed band size: 60 kDa). kappa Opioid Receptor Antibody (YA3132) can be used for WB, IP experiment in rat background.

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