ChemicalBook CAS DataBase List Orvepitant maleate

Orvepitant maleate

Product NameOrvepitant maleate
CAS579475-24-4
CBNumberCB83146347
MFC35H39F7N4O6
MW744.6961824
MDL NumberMFCD20926416
MOL File579475-24-4.mol
MSDS FileSDS

Chemical Properties

solubility	Acetonitrile: Slightly Soluble: 0.1-1 mg/ml Chloroform: Slightly Soluble: 0.1-1 mg/ml
form	Solid
color	Off-white to light yellow
FDA UNII	HAX0H28B6W

Orvepitant maleate Price

Product number	Packaging	Price	Product description	Buy
Cayman Chemical 43077	1mg	$72	Orvepitant (maleate) ≥98%	Buy
Cayman Chemical 43077	5mg	$323	Orvepitant (maleate) ≥98%	Buy
Cayman Chemical 43077	10mg	$466	Orvepitant (maleate) ≥98%	Buy
Biosynth EYA47524	25mg	$1281	Orvepitant maleate	Buy
Biosynth EYA47524	50mg	$1782.5	Orvepitant maleate	Buy

Orvepitant maleate Chemical Properties,Usage,Production

Uses

Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi 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[1][2].

in vivo

Orvepitant (Compound 3a; 0.3-10 mg/kg; Oral administration; marmoset) treatment shows a dose dependant reduction of the number of postures was observed at 1 mg/kg (34.9% reduction), 3 mg/kg (36.6% reduction) and 10 mg/kg (46.4% reduction), suggesting a potential anxiolytic-like effect of the compound^[1].
Orvepitant (compound 3a) shows an oral bioavailability (F) of 17% in rat and 55% in dog, plasma clearance (Clp) of 29 mL/min/kg in rat and 6 mL/min/kg in dog and a half-life of 2.3 h in rat and 6.1 h in dog. As far as the brain penetration in rats is concerned, a B/P ratio of 1.2 is observed 5 min after the i.v. administration of a 1 mg/kg dose of Orvepitant^[1].

Animal Model:	Human threat test in the marmoset (HTT)^[1]
Dosage:	0.3 mg/kg, 1 mg/kg, 3 mg/kg and 10 mg/kg
Administration:	Oral administration
Result:	A dose dependant reduction of the number of postures was observed at 1 mg/kg (34.9% reduction), 3 mg/kg (36.6% reduction) and 10 mg/kg (46.4% reduction).

IC 50

NK1: 10.2 (pKi)

References

[1] Di Fabio R, et al. Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate. Bioorg Med Chem. 2013 Nov 1;21(21):6264-73. DOI:10.1016/j.bmc.2013.09.001
[2] Smith J, et al. The Neurokinin-1 Receptor Antagonist Orvepitant Is a Novel Antitussive Therapy for Chronic Refractory Cough: Results From a Phase 2 Pilot Study (VOLCANO-1). Chest. 2020 Jan;157(1):111-118. DOI:10.1016/j.chest.2019.08.001
[3] MICHAEL K. TROWER. Neurokinin-1 receptor antagonist orvepitant is an effective inhibitor of itch-associated response in a Mongolian gerbil model of scratching behaviour[J]. Experimental Dermatology, 2014, 23 11: 858-860. DOI: 10.1111/exd.12528

Orvepitant maleate synthesis

Preparation Products And Raw materials

Orvepitant maleate Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
BOC Sciences	1-631-485-4226; 16314854226	info@bocsci.com	United States	9920	65
Shanghai Lollane Biological Technology Co.,Ltd.	021-52996696，15000506266 15000506266		China	4865	55
Shanghai EFE Biological Technology Co., Ltd.	021-65675885 18964387627	info@efebio.com	China	9799	58
TargetMol Chemicals Inc.	+1-781-999-5354; +1-00000000000	marketing@targetmol.com	United States	32431	58
cjbscvictory	13348960310 13348960310	3003867561@qq.com	China	10233	58
Hangzhou FuRun Pharmaceutical Technology Co., Ltd	15658004993	1900830611@qq.com	China	980	58
NewCan Biotech Limited	+86-0571-86912261 +86-15658003402	sales@newcanbio.com	China	2087	58
Wuhan Yingnuo Pharmaceutical Technology Co., Ltd.	+86-027-59232304 15387063101	1276242629@qq.com	China	9974	58
TargetMol Chemicals Inc.	4008200310 15002144251	marketing@tsbiochem.com	China	24951	58
Xianning Shen Lan Biomedical Research and Development Co., Ltd.	18171815831	1341138380@qq.com	China	4574	58

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