Orvepitant maleate
- CAS No.
- 579475-24-4
- Chemical Name:
- Orvepitant maleate
- Synonyms
- GW823296 maleate;Orvepitant maleate
- CBNumber:
- CB83146347
- Molecular Formula:
- C35H39F7N4O6
- Molecular Weight:
- 744.6961824
- MDL Number:
- MFCD20926416
- MOL File:
- 579475-24-4.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| Orvepitant (maleate) ≥98% | 43077 | 1mg | $72 |
| Orvepitant (maleate) ≥98% | 43077 | 5mg | $323 |
| Orvepitant (maleate) ≥98% | 43077 | 10mg | $466 |
| Orvepitant maleate | EYA47524 | 25mg | $1281 |
| Orvepitant maleate | EYA47524 | 50mg | $1782.5 |
| 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 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS07,GHS08 |
|---|---|
| Signal word | Danger |
| Hazard statements | H302-H361 |
| Precautionary statements | P264-P270-P301+P312-P330-P501-P201-P202-P281-P308+P313-P405-P501 |
Orvepitant maleate price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 43077 | Orvepitant (maleate) ≥98% | 579475-24-4 | 1mg | $72 | 2026-04-30 | Buy |
| Cayman Chemical | 43077 | Orvepitant (maleate) ≥98% | 579475-24-4 | 5mg | $323 | 2026-04-30 | Buy |
| Cayman Chemical | 43077 | Orvepitant (maleate) ≥98% | 579475-24-4 | 10mg | $466 | 2026-04-30 | Buy |
| Biosynth | EYA47524 | Orvepitant maleate | 579475-24-4 | 25mg | $1281 | 2026-06-04 | Buy |
| Biosynth | EYA47524 | Orvepitant maleate | 579475-24-4 | 50mg | $1782.5 | 2026-06-04 | Buy |
Orvepitant maleate Chemical Properties,Uses,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 Preparation Products And Raw materials
Orvepitant maleate Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32468 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 52923 | 58 | |
| 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 | 9804 | 58 |
| cjbscvictory | 13348960310 13348960310 | 3003867561@qq.com | China | 10235 | 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 | 1785 | 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 | 24960 | 58 |
