NK1 Antagonist

NK1 Antagonists (22):

Cat. No.	Product Name	Effect	Purity

HY-14751

Rolapitant	Antagonist	98.65%
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-10053

Maropitant	Antagonist	99.52%
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-14405A

Casopitant mesylate	Antagonist	99.84%
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. 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-12143

Vofopitant dihydrochloride	Antagonist	99.11%
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-10049A

CP 122721 hydrochloride	Antagonist
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-122347A

Orvepitant maleate	Antagonist	99.99%
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-P0061

Vapreotide	Antagonist	98.06%
Vapreotide is a neurokinin-1 (NK1) receptor antagonist, with an IC₅₀ of 330 nM.

HY-P1194

Spantide I	Antagonist	99.85%
Spantide I, a substance P analog, is a selective NK₁ receptor antagonist, with K_i values of 230 nM and 8150 nM for NK₁ and NK₂ receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.

HY-151413

MEN 10207	Antagonist	99.58%
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-P0061A

Vapreotide acetate	Antagonist	99.67%
Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) is a neurokinin-1 (NK1) receptor antagonist, with an IC₅₀ of 330 nM.

HY-P1722

Spantide II	Antagonist	98.01%
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-108479

Nolpitantium	Antagonist
Nolpitantium (SR140333) is a potent, selective, competitive, non-peptide tachykinin NK₁ receptor antagonist. Nolpitantium blocks the activation of rat thalamic neurons after nociceptive stimulation.

HY-16436

Rolapitant hydrochloride hydrate	Antagonist	98.25%
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-133206A

Fosnetupitant chloride monohydrochloride	Antagonist	99.70%
Fosnetupitant chloride monohydrochloride (Pronetupitant chloride monohydrochloride) is an NK1 antagonist with pK_i values of 9.5, 6.1 for human NK1 and NK3 receptor, respectively. Fosnetupitant chloride monohydrochloride is a methylene phosphate prodrug of Netupitant.

HY-108480

SDZ NKT 343	Antagonist
SDZ NKT 343 is a selective, orally active NK₁ receptor antagonist with an IC₅₀ of 0.62 nM against human NK₁ receptor. SDZ NKT 343 has good analgesic activity.

HY-19633

CS-003 Free base	Antagonist
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-P3802

[D-Trp2,7,9] Substance P	Antagonist
[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-109147

Imnopitant	Antagonist
Imnopitant is a NK1 receptor antagonist (WO2020132716, compound 1) .

HY-14751A

Rolapitant hydrochloride	Antagonist
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-108481

L-760735	Antagonist
L-760735 is a high affinity, selective and orally active NK1 receptor antagonist with an IC₅₀ of 0.19 nM for human NK1 receptors. L-760735 exhibits anxiolytic and antidepressant-like effects.

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