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neurokinin NK1 receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Neurokinin Receptor (42) Caspase (1) Cytochrome P450 (2) Endogenous Metabolite (2) Interleukin Related (1) Isotope-Labeled Compounds (1) Mitochondrial Metabolism (1)
By Research Areas:	Cancer (12) Endocrinology (11) Infection (2) Inflammation/Immunology (6) Metabolic Disease (1) Neurological Disease (34)
Click Chemistry:	Alkynes (1)

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Targets Recommended: Neurokinin Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P0061

Vapreotide 1 Publications Verification RC160; BMY 41606	Neurokinin Receptor	Cancer
Vapreotide is a **neurokinin-1 (NK1) receptor** antagonist, with an IC₅₀ of 330 nM.

HY-P0061A

Vapreotide acetate 1 Publications Verification RC-160 acetate; BMY-41606 acetate	Neurokinin Receptor	Cancer
Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) is a **neurokinin-1 (NK1) receptor** antagonist, with an IC₅₀ of 330 nM.

HY-101249

L-732138	Neurokinin Receptor	Neurological Disease Cancer
L-732138 is a selective, potent and competitive **neurokinin-1 (NK-1) receptor** antagonist with an IC₅₀ of 2.3 nM. L-732138 has 200-fold more potent in cloned human **NK-1 receptors than cloned rat NK-1 receptors*, and has > 1000-fold more potent than human NK-2 and NK-3 receptors*. L-732138 can reduce hyperalgesia and has antitumor action .

HY-109147A

Imnopitant dihydrochloride	Neurokinin Receptor	Neurological Disease
Imnopitant dihydrochloride is a neurokinin **NK1 receptor** antagonist .

HY-12114

Serlopitant VPD-737; MK-0594	Neurokinin Receptor	Neurological Disease Endocrinology
Serlopitant is a selective **Neurokinin-1 (NK-1)** receptor antagonist.

HY-105346

WIN 51708	Neurokinin Receptor	Neurological Disease
WIN 51708 is a nonpeptide antagonist of **neurokinin (NK)-1 receptor*. WIN 51708 has a higher affinity for the rat NK-1* receptor compared to the human NK-1 receptor .

HY-P0061B

Vapreotide diacetate RC160 diacetate; BMY 41606 diacetate	Neurokinin Receptor	Cancer
Vapreotide diacetate is a **neurokinin-1 (NK1) receptor** antagonist, with an IC₅₀ of 330 nM.

HY-159842

Fosrolapitant	Neurokinin Receptor	Neurological Disease
Fosrolapitant is a **neurokinin 1 (NK1) receptor** antagonist .

HY-19665

Lanepitant LY303870	Neurokinin Receptor	Neurological Disease Inflammation/Immunology
Lanepitant (LY303870) is a selective neurokinin-1 (NK-1) receptor antagonist. Lanepitant blocks neurogenic inflammation and pain transmission by preventing the binding of substance P to *NK-1* receptors on both neuronal and non-neuronal tissues. Lanepitant can be used to study osteoarthritis .

HY-105436

FR 113680	Neurokinin Receptor	Neurological Disease
FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK₁ neurokinin receptor .

HY-108483

RP 67580	Neurokinin Receptor	Neurological Disease Inflammation/Immunology
RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a K_i value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation .

HY-18006

NKP608 1 Publications Verification	Neurokinin Receptor	Neurological Disease Endocrinology
NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo.

HY-16346S

Netupitant-d6 CID-6451149-d₆	Neurokinin Receptor	Neurological Disease Endocrinology
Netupitant-d₆ is the deuterium labeled Netupitant (CID-6451149), which is a highly potent and selective, orally active neurokinin-1 (NK1) receptor antagonist[1].

HY-10049A

CP 122721 hydrochloride	Neurokinin Receptor	Neurological Disease
CP 122721 hydrochloride is a potent, non-peptide and selective nonpeptide **neurokinin NK1** antagonist, with a pIC₅₀ of 9.8 for human NK1 receptor expressed in IM-9 cells. CP 122721 hydrochloride exhibits anxiolytic and antidepressant-like effects .

HY-12143

Vofopitant dihydrochloride GR 205171A	Neurokinin Receptor	Neurological Disease Endocrinology Cancer
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [ ³H]SP binding to the NK1 receptor with pK_i values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent .

HY-P10588

WIN 66306	Neurokinin Receptor	Others
WIN 66306 is a cyclic heptapeptide that can be isolated from an Aspergillus species. WIN 66306 is a neurokinin antagonist with antagonistic effects on both *NK1* and NK2 receptors .

HY-122347A

Orvepitant maleate GW823296 maleate	Neurokinin Receptor	Neurological Disease
Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated **neurokinin-1 receptor (NK-1)** antagonist with a pK_i of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment .

HY-118463

Benzomalvin A	Neurokinin Receptor	Neurological Disease
Benzomalvin A is a potent antagonist of **neurokinin receptor** isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with K_i values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively .

HY-16346

Netupitant 3 Publications Verification CID 6451149	Neurokinin Receptor	Neurological Disease Endocrinology Cancer
Netupitant (CID-6451149) is a highly potent, selective and orally active **neurokinin-1 (NK₁)** receptor antagonist with a K_i of 0.95 nM for hNK₁ in CHO cells. Netupitant has antiemetic affect .

HY-17012

Dapitant RPR 100893	Neurokinin Receptor	Inflammation/Immunology
Dapitant (RPR 100893) is a non-peptide Substance P antagonist with high affinity for the human NK1 receptor. It belongs to the 7,7,4-trimethylperhydroisoindole class of compounds. Dapitant inhibits the binding of Substance P to NK1 receptors, thereby blocking its neurokinin-mediated effects. This novel antagonist represents a potential therapeutic option for conditions involving Substance P, such as neurogenic inflammation and pain modulation .

HY-119552

Acetylaszonalenin LL-S490β	Endogenous Metabolite Neurokinin Receptor	Neurological Disease
Acetylaszonalenin, a prenylated indole derivative, is a fungal metabolite.Acetylaszonalenin is a potent **neurokinin-1 (NK1)** receptor antagonist. Acetylaszonalenin shows inhibition of [ ³H]-SP binding to human astrocytoma cells with a K_i of 170 μM .

HY-P3802

[D-Trp2,7,9] Substance P	Neurokinin Receptor	Neurological Disease
[D-Trp2,7,9] Substance P is a tachykinin (Neurokinin *Receptor) antagonist* with K_i values of 1 μM, 1.3 μM, and ~9 μM for *NK-1, NK-2,and NK-3* receptor, respectively .

HY-106982

Ezlopitant CJ-11,974	Neurokinin Receptor	Neurological Disease Metabolic Disease
Ezlopitant (CJ-11,974) is a selective, non-peptidic **neurokinin-1 (NK-1)-receptor** antagonist. Ezlopitant inhibits both acute and delayed emetic reactions induced by Cisplatin (HY-17394) in ferrets via acting on NK1 receptors in the central nervous system. Ezlopitant has the potential for pain, chemotherapy-induced emesis and irritable bowel syndrome research .

HY-151413

MEN 10207	Neurokinin Receptor	Neurological Disease
MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.

HY-10053

Maropitant	Neurokinin Receptor	Neurological Disease Endocrinology
Maropitant is a selective and orally active **neurokinin (NK1) receptor** antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting .

HY-16346R

Netupitant (Standard)	Neurokinin Receptor	Neurological Disease Endocrinology
Netupitant (Standard) is the analytical standard of Netupitant. This product is intended for research and analytical applications. Netupitant (CID-6451149) is a highly potent, selective and orally active **neurokinin-1 (NK₁)** receptor antagonist with a K_i of 0.95 nM for hNK₁ in CHO cells. Netupitant has antiemetic affect .

HY-118378

ZD6021	Neurokinin Receptor	Neurological Disease Endocrinology
ZD6021 is an orally active **Neurokinin 1 Receptor** antagonist, with K_i values of 0.12 nM for *NK1* and 0.62 nM for NK2. At a concentration of 100 nM, ZD6021 has a pK_B value of 8.9 for human pulmonary artery *NK1* receptors, and a pK_B value of 7.3 for human bronchial NK2 receptors. ZD6021 effectively reduces ASMSP-induced plasma protein extravasation in guinea pigs, with an ED₅₀ of 0.5 mg/kg, and also decreases NK2 mediated bronchoconstriction, with an ED₅₀ of 13 mg/kg .

HY-14751

Rolapitant SCH619734	Neurokinin Receptor	Neurological Disease Cancer
Rolapitant (SCH619734) is a potent, selective, long-acting and orally active **neurokinin 1 (NK1) receptor** antagonist with a K_i of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model .

HY-14751A

Rolapitant hydrochloride SCH619734 hydrochloride	Neurokinin Receptor	Neurological Disease Cancer
Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active **neurokinin 1 (NK1) receptor** antagonist with a K_i of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model .

HY-16436

Rolapitant hydrochloride hydrate SCH619734 hydrochloride hydrate	Neurokinin Receptor	Neurological Disease Cancer
Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active **neurokinin 1 (NK1) receptor** antagonist with a K_i of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model .

HY-19633

CS-003 Free base	Neurokinin Receptor	Infection Endocrinology
CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with K_i values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. CS-003 Free base (CS-003) has therapeutic efficacy on respiratory diseases associated with neurokinins.

HY-117952

L 743310	Neurokinin Receptor	Neurological Disease
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 guinea pig esophagus. L 743310 has a dose-dependent inhibitory effect on cisplatin-induced emesis .

HY-10053S1

Maropitant-13C,d3	Isotope-Labeled Compounds Neurokinin Receptor	Neurological Disease Endocrinology
Maropitant- ¹³C,d₃ is the ¹³C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting[1][2].

HY-116620

Benzomalvin C	Neurokinin Receptor	Infection
Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor inhibiting binding of substance P by 46% when used at 100 μg/mL in vitro. It is also a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC₅₀ value of 130 μM for recombinant IDO. It is isolated from Penicillium and contains an epoxide group at C-19 and C-20, which is not present in benzomalvins A, B, or E.

HY-14751R

Rolapitant (Standard)	Neurokinin Receptor	Neurological Disease Cancer
Rolapitant (Standard) is the analytical standard of Rolapitant. This product is intended for research and analytical applications. Rolapitant (SCH619734) is a potent, selective, long-acting and orally active **neurokinin 1 (NK1) receptor** antagonist with a K_i of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model .

HY-120167

YM-44778	Neurokinin Receptor	Neurological Disease Inflammation/Immunology
YM-44778 is a **neurokinin receptor** antagonist. The _pK_i values for NK1, NK2 and NK3 are 8.08, 8.55 and 8.24, respectively. YM-44778 inhibits the increase of bladder pressure induced by substance [Sar9,Met(O2)11] -P (HY-P1012) in anestheticized rats .

HY-14405

Casopitant GW679769	Neurokinin Receptor Cytochrome P450	Neurological Disease
Casopitant (GW679769) is a potent, selective, brain-penetrant and orally active neurokinin 1 (NK₁) receptor antagonist. Casopitant antagonizes the emetic effects of Substance P (HY-P0201). Casopitant is also a substrate and weak to moderate inhibitor of CYP3A4. Casopitant is indicated for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV) .

HY-14405A

Casopitant mesylate GW679769B	Neurokinin Receptor Cytochrome P450	Neurological Disease Cancer
Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active **neurokinin 1 (NK1) receptor** antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of Substance P (HY-P0201). Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV) .

HY-107691

GR 159897	Neurokinin Receptor	Neurological Disease Endocrinology Cancer
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide **neurokinin 2 (NK₂) receptor** antagonist. GR 159897 has little or no affinity for NK₁ and NK₃ receptors. GR 159897 inhibits binding of [ ³H]GR100679 to human NK₂ (hNK₂)-CHO cells and rat colon membranes with pK_is of 9.51 and 10, respectively. Antagonizes bronchoconstriction. Anxiolytic-like and anti-tumor effects .

HY-P1722

Spantide II	Neurokinin Receptor	Inflammation/Immunology
Spantide II, an undecapeptide substance P (SP) analog, is a potent **neurokinin-1 receptor (NK-1R)** antagonist. Spantide II binds with NK-1R and blocks proinflammatory activities associated with SP. Spantide II can be used in the research of inflammatory skin disorders, such as psoriasis and contact dermatitis .

HY-P3854

GR 83074	Neurokinin Receptor	Neurological Disease
GR 83074 is a potent and selective NK-2 (Neurokinin *Receptor) antagonist* with a pK_B of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity .

HY-W011978

N-Acetyl-L-tryptophan	Endogenous Metabolite Mitochondrial Metabolism Neurokinin Receptor Caspase Interleukin Related	Neurological Disease Inflammation/Immunology
N-Acetyl-L-tryptophan is an antagonist of the neurokinin-1 receptor (NK-1R), disrupting the binding of substance P (SP) to *NK-1R. This action provides neuroprotective effects, improving memory deficits and motor impairments. N-Acetyl-L-tryptophan is also an inhibitor of cytochrome c (Cytochrome c), and it exerts antioxidant and anti-inflammatory effects by inhibiting the expression of IL-1β* and the activation of caspase-1. N-Acetyl-L-tryptophan holds promise for research in neurodegenerative and inflammatory diseases .

Cat. No.	Product Name	Target	Research Area

HY-P0061

Vapreotide 1 Publications Verification RC160; BMY 41606	Neurokinin Receptor	Cancer
Vapreotide is a **neurokinin-1 (NK1) receptor** antagonist, with an IC₅₀ of 330 nM.

HY-P0061A

Vapreotide acetate 1 Publications Verification RC-160 acetate; BMY-41606 acetate	Neurokinin Receptor	Cancer
Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) is a **neurokinin-1 (NK1) receptor** antagonist, with an IC₅₀ of 330 nM.

HY-151413

MEN 10207	Neurokinin Receptor	Neurological Disease
MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.

HY-P1722

Spantide II	Neurokinin Receptor	Inflammation/Immunology
Spantide II, an undecapeptide substance P (SP) analog, is a potent **neurokinin-1 receptor (NK-1R)** antagonist. Spantide II binds with NK-1R and blocks proinflammatory activities associated with SP. Spantide II can be used in the research of inflammatory skin disorders, such as psoriasis and contact dermatitis .

HY-P0061B

Vapreotide diacetate RC160 diacetate; BMY 41606 diacetate	Neurokinin Receptor	Cancer
Vapreotide diacetate is a **neurokinin-1 (NK1) receptor** antagonist, with an IC₅₀ of 330 nM.

HY-105436

FR 113680	Neurokinin Receptor	Neurological Disease
FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK₁ neurokinin receptor .

HY-P10588

WIN 66306	Neurokinin Receptor	Others
WIN 66306 is a cyclic heptapeptide that can be isolated from an Aspergillus species. WIN 66306 is a neurokinin antagonist with antagonistic effects on both *NK1* and NK2 receptors .

HY-P3802

[D-Trp2,7,9] Substance P	Neurokinin Receptor	Neurological Disease
[D-Trp2,7,9] Substance P is a tachykinin (Neurokinin *Receptor) antagonist* with K_i values of 1 μM, 1.3 μM, and ~9 μM for *NK-1, NK-2,and NK-3* receptor, respectively .

HY-P3854

GR 83074	Neurokinin Receptor	Neurological Disease
GR 83074 is a potent and selective NK-2 (Neurokinin *Receptor) antagonist* with a pK_B of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-W011978

N-Acetyl-L-tryptophan	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Source classification Metabolic Disease Endogenous metabolite Disease Research Fields	Endogenous Metabolite Mitochondrial Metabolism Neurokinin Receptor Caspase Interleukin Related
N-Acetyl-L-tryptophan is an antagonist of the neurokinin-1 receptor (NK-1R), disrupting the binding of substance P (SP) to *NK-1R. This action provides neuroprotective effects, improving memory deficits and motor impairments. N-Acetyl-L-tryptophan is also an inhibitor of cytochrome c (Cytochrome c), and it exerts antioxidant and anti-inflammatory effects by inhibiting the expression of IL-1β* and the activation of caspase-1. N-Acetyl-L-tryptophan holds promise for research in neurodegenerative and inflammatory diseases .

HY-118463

Benzomalvin A	Alkaloids Human Gut Microbiota Metabolites Microorganisms Source classification Quinoline Alkaloids Endogenous metabolite	Neurokinin Receptor
Benzomalvin A is a potent antagonist of **neurokinin receptor** isolated from Penicillium sp. Benzomalvin A shows inhibitory activity against substance P with K_i values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively .

HY-119552

Acetylaszonalenin LL-S490β	Alkaloids Microorganisms Source classification Indole Alkaloids	Endogenous Metabolite Neurokinin Receptor
Acetylaszonalenin, a prenylated indole derivative, is a fungal metabolite.Acetylaszonalenin is a potent **neurokinin-1 (NK1)** receptor antagonist. Acetylaszonalenin shows inhibition of [ ³H]-SP binding to human astrocytoma cells with a K_i of 170 μM .

HY-116620

Benzomalvin C	Human Gut Microbiota Metabolites Microorganisms Source classification Endogenous metabolite	Neurokinin Receptor
Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor inhibiting binding of substance P by 46% when used at 100 μg/mL in vitro. It is also a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC₅₀ value of 130 μM for recombinant IDO. It is isolated from Penicillium and contains an epoxide group at C-19 and C-20, which is not present in benzomalvins A, B, or E.

Cat. No.	Product Name	Chemical Structure

HY-16346S

Netupitant-d6
Netupitant-d₆ is the deuterium labeled Netupitant (CID-6451149), which is a highly potent and selective, orally active neurokinin-1 (NK1) receptor antagonist[1].

HY-10053S1

Maropitant-13C,d3
Maropitant- ¹³C,d₃ is the ¹³C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting[1][2].

Cat. No.	Product Name		Classification

HY-105346

WIN 51708		Alkynes
WIN 51708 is a nonpeptide antagonist of **neurokinin (NK)-1 receptor*. WIN 51708 has a higher affinity for the rat NK-1* receptor compared to the human NK-1 receptor .

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neurokinin NK1 receptor antagonist

Inhibitors & Agonists

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Isotope-Labeled Compounds

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