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neurokinin receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Neurokinin Receptor (86) Antibiotic (3) Apoptosis (1) Bacterial (3) Bcl-2 Family (1) Cadherin (1) Calcium Channel (1) Caspase (3) Cyclin G-associated Kinase (GAK) (1) Cytochrome P450 (2) Drug Metabolite (1) Endogenous Metabolite (6) HIV (3) Interleukin Related (2) Isotope-Labeled Compounds (6) Mitochondrial Metabolism (2) p38 MAPK (2) Reference Standards (7) VEGFR (1) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (24) Endocrinology (25) Infection (2) Inflammation/Immunology (14) Metabolic Disease (4) Neurological Disease (69)
Click Chemistry:	Alkynes (1)

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Isotope-Labeled Compounds

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Targets Recommended: Neurokinin Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10052

Aprepitant Maximum Cited Publications 13 Publications Verification MK-0869; MK-869; L-754030	Neurokinin Receptor Bacterial HIV Antibiotic	Neurological Disease Endocrinology Cancer
Aprepitant (MK-0869) is a selective and high-affinity **neurokinin 1 receptor** antagonist with a K_d of 86 pM.

HY-19632

Fezolinetant 5 Publications Verification ESN-364	Neurokinin Receptor	Endocrinology
Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.

HY-16346

Netupitant 4 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-14751

Rolapitant SCH619734	Neurokinin Receptor	Neurological Disease
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-14407A

Fosaprepitant dimeglumine 3 Publications Verification MK-0517; L785298	Neurokinin Receptor	Neurological Disease Endocrinology Cancer
Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a **neurokinin-1 receptor** antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .

HY-14432

Pavinetant 3 Publications Verification MLE-4901; AZD2624; AZD4901	Neurokinin Receptor	Neurological Disease Endocrinology
Pavinetant (MLE-4901) is a **neurokinin-3 receptor (NK3R*) antagonist*.

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 .

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-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-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-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-14406A

L-733060 hydrochloride 1 Publications Verification	Neurokinin Receptor	Neurological Disease Cancer
L-733060 hydrochloride is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 hydrochloride mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 hydrochloride blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 hydrochloride reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 hydrochloride can be used for the study of chronic orofacial pain .

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-122347A

Orvepitant maleate GW823296 maleate	Neurokinin Receptor	Neurological Disease Inflammation/Immunology
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-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-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-P1722

Spantide II 1 Publications Verification	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-117380

SB 235375	Neurokinin Receptor	Neurological Disease
SB 235375 is a potent and selective antagonist of the human neurokinin-3 (hNK-3) receptor designed by optimizing the structure of 2-phenyl-4-quinolinecarboxylic acid amide. SB 235375 displays high affinity for the hNK-3 receptor, with significantly higher binding affinities than hNK-2 and hNK-1 receptors. In vitro studies demonstrated its ability to block NK-3 receptor-mediated contraction and calcium mobilization, while in vivo, SB 223412 demonstrated oral and intravenous activity against NK-3 receptor-driven responses in animal models .

HY-18006

NKP608 1 Publications Verification	Neurokinin Receptor Wnt Bcl-2 Family β-catenin Cyclin G-associated Kinase (GAK) VEGFR Caspase Cadherin Apoptosis	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
NKP608 is a non-peptidic derivative of 4-aminopiperidine, a highly selective, orally active, neurokinin-1 (NK₁) receptor antagonist with IC₅₀ of 2.6 nM. NKP608 is active both in vitro and in vivo, showing extremely low affinity for NK₂, NK₃ receptors. NKP608 exerts its effects by blocking the NK₁ receptor, regulate cell proliferation and apoptosis, affect neurotransmitter functions and gastric mucosal repair mechanisms, and suppress the Wnt/β-catenin pathway in antitumor research. NKP608 is applicable to research related to various diseases, including cough, anxiety disorders, depression, gastric mucosal injury, and colorectal cancer .

HY-151413

MEN 10207 1 Publications Verification	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-P1276A

Men 10376 TFA 1 Publications Verification neurokinin-2 receptor antagonist TFA	Neurokinin Receptor	Endocrinology
Men 10376 TFA is a selective tachykinin NK-2 receptor antagonist, with a K_i of 4.4 μM for rat small intestine NK-2 receptor .

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 .

HY-14407

Fosaprepitant L-758298	Neurokinin Receptor	Neurological Disease Endocrinology Cancer
Fosaprepitant (L-785298) is a proagent of Aprepitant (HY-10052). Fosaprepitant is a **neurokinin-1 receptor** antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .

HY-10052R

Aprepitant (Standard) MK-0869 (Standard); MK-869 (Standard); L-754030 (Standard)	Reference Standards Neurokinin Receptor Bacterial HIV Antibiotic	Neurological Disease Endocrinology Cancer
Aprepitant (Standard) is the analytical standard of Aprepitant. This product is intended for research and analytical applications. Aprepitant (MK-0869) is a selective and high-affinity **neurokinin 1 receptor** antagonist with a K_d of 86 pM.

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-P3850

(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B	Neurokinin Receptor	Neurological Disease
(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B is a competitive antagonist of Neurokinin B (Neurokinin *Receptor) with a pA2 of 5.5. (D-Pro2,D-Trp6,8,Nle10)-Neurokinin* B shows no influence on Substance P or Neurokinin A .

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-P3598

Substance P(1-4)	Neurokinin Receptor	Cancer
Substance P(1-4) is a potent neurokinin receptors (NK-R) antagonist. Substance P(1-4) has regulation of normal hematopoiesis and inhibits endogenous erythroid colony (EEC) formation .

HY-178269

SCH-720881	Drug Metabolite Neurokinin Receptor	Neurological Disease
SCH-720881 is the active metabolite of Rolapitant (HY-14751). 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-12144

CP-99994	Neurokinin Receptor p38 MAPK	Neurological Disease
CP-99994 is a Tachykinin neurokinin 1 (NK-1) receptor antagonist with a K_i of 0.25 nM. CP-99994 prevents colorectal sensitization in the context of visceral hypersensitivity. CP-99994 reduces colorectal hypersensitivity induced by acetic acid injections in a model of bladder-colon cross-sensitization. CP-99994 hydrochloride attenuates the neuroglial interactions and MAPK-p38 phosphorylation associated with visceral hypersensitivity .

HY-P1276

Men 10376 neurokinin-2 receptor antagonist	Neurokinin Receptor	Endocrinology
Men 10376 is a selective tachykinin NK-2 receptor antagonist, with a K_i of 4.4 μM for rat small intestine NK-2 receptor.

HY-12114

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

HY-109147A

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

HY-14407AS

Fosaprepitant-d4 dimeglumine MK-0517-d₄; L785298-d₄	Isotope-Labeled Compounds Neurokinin Receptor	Neurological Disease Endocrinology Cancer
Fosaprepitant-d₄ (dimeglumine) is deuterium labeled Fosaprepitant (dimeglumine). Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .

HY-116822

SSR 146977	Neurokinin Receptor	Neurological Disease
SSR 146977 is a potent and selective antagonist of the tachykinin NK3 receptor. SSR 146977 inhibits the binding of radioactive neurokinin B to NK3 receptors in Chinese hamster ovary cells, with a K_i of 0.26 nM .

HY-14407AR

Fosaprepitant dimeglumine (Standard) MK-0517 (Standard); L785298 (Standard)	Reference Standards Neurokinin Receptor	Neurological Disease Endocrinology Cancer
Fosaprepitant (dimeglumine) (Standard) is the analytical standard of Fosaprepitant (dimeglumine). This product is intended for research and analytical applications. Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a **neurokinin-1 receptor** antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .

HY-105462

MDL 105212A	Neurokinin Receptor	Neurological Disease Inflammation/Immunology
MDL 105212A is a potent and orally active nonpeptide **neurokinin receptor (NK-1/NK-2*) tachykinin receptor* antagonist. MDL 105212A can be used for the researches of inflammation, immunology and neurological disease, such as asthma .

HY-10050

CJ-17493	Neurokinin Receptor	Neurological Disease
CJ-17493 is a neurokinin-1 (NK1) receptor antagonist, with a K_i of 0.2 nM. CJ-17493 shows moderate affinity for the verapamil-binding site of L-type Ca ²⁺ channels (IC₅₀ = 164 nM) and site 2 of sodium channels (IC₅₀ = 48 nM). CJ-17493 can be used for the study of neurological diseases .

HY-128537

DNK-333	Neurokinin Receptor	Inflammation/Immunology
DNK-333 is a potent and balanced dual NK1 and NK2 receptor antagonist with IC₅₀ values of 4.8 nM and 5.5 nM, respectively. DNK-333 blocks the Neurokinin A (NKA) (HY-P0197)-induced bronchoconstriction in asthma .

HY-10053S

Maropitant-d3	Isotope-Labeled Compounds Neurokinin Receptor	Neurological Disease Endocrinology
Maropitant-d₃ is the 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 .

HY-14406

L-733060	Neurokinin Receptor	Neurological Disease Cancer
L-733060 is a selective neurokinin-1 (NK-1) receptor antagonist. L-733060 mainly regulates pain transmission and neural plasticity by blocking the binding of Substance P (P substance) to the NK-1 receptor. L-733060 blocks the promoting effect of Substance P on long-term potentiation (LTP) in the hippocampus. L-733060 reverses the orofacial hyperalgesia induced by experimental occlusal interference (EOI) in rats. L-733060 hydrochloride inhibits neurogenic plasma extravasation at a dose that does not cause adverse cardiovascular effects in rodents, and also acts as an anti-tumor agent. L-733060 can be used for the study of chronic orofacial pain .

HY-W011978S

N-Acetyl-L-tryptophan-d3	Isotope-Labeled Compounds Endogenous Metabolite Mitochondrial Metabolism Neurokinin Receptor Caspase Interleukin Related	Neurological Disease Inflammation/Immunology
N-Acetyl-L-tryptophan-d₃ is the deuterium labeled N-Acetyl-L-tryptophan (HY-W011978). 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-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-19429A

SLV-317	Neurokinin Receptor	Neurological Disease
SLV-317 is an antagonist of the **neurokinin-1 receptor** with oral activity. SLV-317 can effective antagonist of substance P-induced effects .

HY-159842

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

HY-105137

Lanepitant dihydrochloride LY303870 dihydrochloride	Neurokinin Receptor	Neurological Disease Inflammation/Immunology
Lanepitant dihydrochloride (LY303870 dihydrochloride) is a non-peptide *neurokinin-1* receptor antagonist. Lanepitant dihydrochloride has analgesic and anti-inflammatory activities .

HY-19429

SLV-317 free base	Neurokinin Receptor	Metabolic Disease
SLV-317 (free base) is an antagonist of the **neurokinin-1 receptor** with oral activity. SLV-317 (free base) can effective antagonist of substance P-induced effects .

HY-19633A

CS-003	Endogenous Metabolite	Neurological Disease
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, withK_i values of 2.3 nM, 0.54 nM and 0.74 nM respectively. The K_i values of CS-003 on the guinea pig 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 .

HY-122347

Orvepitant GW823296	Neurokinin Receptor	Neurological Disease Cancer
Orvepitant (GW823296) 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 can across the blood-brain barrier. Orvepitant has the potential for depressive disorder and chronic refractory cough (CRC) treatment .

HY-14432R

Pavinetant (Standard) MLE-4901 (Standard); AZD2624 (Standard); AZD4901 (Standard)	Neurokinin Receptor Reference Standards	Neurological Disease Endocrinology
Pavinetant (Standard) is the analytical standard of Pavinetant. This product is intended for research and analytical applications. Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.

Cat. No.	Product Name	Target	Research Area

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-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-P1722

Spantide II 1 Publications Verification	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-151413

MEN 10207 1 Publications Verification	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-P1276A

Men 10376 TFA 1 Publications Verification neurokinin-2 receptor antagonist TFA	Neurokinin Receptor	Endocrinology
Men 10376 TFA is a selective tachykinin NK-2 receptor antagonist, with a K_i of 4.4 μM for rat small intestine NK-2 receptor .

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-P3850

(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B	Neurokinin Receptor	Neurological Disease
(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B is a competitive antagonist of Neurokinin B (Neurokinin *Receptor) with a pA2 of 5.5. (D-Pro2,D-Trp6,8,Nle10)-Neurokinin* B shows no influence on Substance P or Neurokinin A .

HY-P3598

Substance P(1-4)	Neurokinin Receptor	Cancer
Substance P(1-4) is a potent neurokinin receptors (NK-R) antagonist. Substance P(1-4) has regulation of normal hematopoiesis and inhibits endogenous erythroid colony (EEC) formation .

HY-P1276

Men 10376 neurokinin-2 receptor antagonist	Neurokinin Receptor	Endocrinology
Men 10376 is a selective tachykinin NK-2 receptor antagonist, with a K_i of 4.4 μM for rat small intestine NK-2 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-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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-W011978

N-Acetyl-L-tryptophan	Classification of Application Fields Ketones, Aldehydes, Acids Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	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 (-)-Benzomalvin A	Alkaloids Human Gut Microbiota Metabolites Microorganisms Quinoline Alkaloids Endogenous metabolite Source Classification	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 Indole Alkaloids Source Classification	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 Endogenous metabolite Source Classification	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.

HY-N9554

WIN-64821	Structural Classification Microorganisms Ketones, Aldehydes, Acids Source Classification	Neurokinin Receptor Endogenous Metabolite Calcium Channel
WIN-64821 is a secondary metabolite produced by Aspergillus species, and acts as a **Neurokinin Receptor** antagonist. The K_i values of WIN-64821 for NK1, NK2 and NK3 receptors are 0.24 (human astrocytoma cells), 0.26 (rat duodenum) and 15.2 (guinea pig forebrain) μM, respectively. WIN-64821 inhibits apamin-induced contraction of rat vas deferens, blocks substance P-induced contraction of guinea pig ileum and Ca ²⁺ efflux in human astrocytoma cells. WIN-64821 is applicable to analgesic and anti-inflammatory research .

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 .

HY-14407AS

Fosaprepitant-d4 dimeglumine
Fosaprepitant-d₄ (dimeglumine) is deuterium labeled Fosaprepitant (dimeglumine). Fosaprepitant dimeglumine (MK-0517) is a proagent of Aprepitant (HY-10052). Fosaprepitant dimeglumine is a neurokinin-1 receptor antagonist, which is development for the prevention of chemotherapy-induced nausea and vomiting (CINV) .

HY-10053S

Maropitant-d3
Maropitant-d₃ is the 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 .

HY-W011978S

N-Acetyl-L-tryptophan-d3

N-Acetyl-L-tryptophan-d₃ is the deuterium labeled N-Acetyl-L-tryptophan (HY-W011978). 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-W777166

Aprepitant-13C2,d2 (Major)
Aprepitant- ¹³C₂,d₂ (Major) (MK-0869- ¹³C₂,d₂) is ¹³C labeled Aprepitant. Aprepitant (MK-0869) is a selective and high-affinity **neurokinin 1 receptor** antagonist with a K_d of 86 pM.

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 .

HY-19632S

Fezolinetant-d4
Fezolinetant-d₄ (ESN-364-d₄) is the deuterium labeled Fezolinetant (HY-19632). Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.

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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