Neurokinin Receptor Antagonist

Neurokinin Receptor Antagonists (123):

Cat. No.	Product Name	Effect	Purity

HY-19632

Fezolinetant	Antagonist	99.19%
Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes.

HY-14407A

Fosaprepitant dimeglumine	Antagonist	98.02%
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-W017933

Octahydroisoindole	Antagonist	99.09%
Octahydroisoindole (Perhydroisoindole) is a substance P antagonist that can cross the blood-brain barrier and is useful for the study of movement disorders associated with central nervous system diseases.

HY-14751

Rolapitant	Antagonist	99.22%
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-16346

Netupitant	Antagonist	99.93%
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-109171

Elinzanetant	Antagonist	99.82%
Elizanetant (NT-814) is an orally active, selective NK-1,3 receptor antagonist. Elizanetant can reduce the levels of estradiol and progesterone, and is used in the study of vascular motor symptoms and sleep disorders related to menopause in women.

HY-106910

Saredutant	Antagonist	98.09%
Saredutant is a selective NK2 receptor antagonist.

HY-15722

SB-222200	Antagonist	99.85%
SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders.

HY-101249

L-732138	Antagonist	≥99.9%
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-14552

Talnetant	Antagonist	99.48%
Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a K_i of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies.

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 (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-14551

Osanetant	Antagonist	98.08%
Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia.

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-135108

QWF Peptide	Antagonist	98.15%
QWF Peptide (Compound 4a) is a substance P antagonist with an IC₅₀ of 0.09 μM. QWF Peptide antagonizes the SP-induced contraction of isolated guinea pig trachea strips with an IC₅₀ of 4.7 μM.

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-14432

Pavinetant	Antagonist	99.83%
Pavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist.

HY-14406A

L-733060 hydrochloride	Antagonist	99.04%
L-733060 hydrochloride is a potent tachykinin NK₁ receptor antagonist. L-733060 hydrochloride inhibits neurogenic plasma extravasation at doses that do not cause adverse cardiovascular effects in rodents and also acts as an antitumoral agent.

HY-P0061

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

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-P1194

Spantide I	Antagonist	99.72%
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.

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