2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. Orvepitant maleate

Orvepitant maleate  (Synonyms: GW823296 maleate)

Cat. No.: HY-122347A Purity: 99.99%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Orvepitant maleate Chemical Structure

Orvepitant maleate Chemical Structure

CAS No. : 579475-24-4

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Orvepitant maleate Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

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].

IC50 & Target[1]

NK1

10.2 (pKi)

In Vitro

Orvepitant (Compound 3a) is further characterized in terms of the ability to functionally inhibit substance P (SP)-induced release of cytosolic Ca2+ in human neurokinin-1 receptor (hNK1)-CHO cells. Orvepitant (0.3-10 nM), pre-incubated for 1 h at 37℃ before adding the agonist SP, produces a non-surmountable antagonism of agonist concentration-response curve. For Orvepitant apparents pKB value of 10.30[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Orvepitant maleate Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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).
Clinical Trial
Molecular Weight

744.70

Appearance

Solid

Formula

C35H39F7N4O6
CAS No.
SMILES

O=C(N1[C@@H](C2=CC=C(F)C=C2C)C[C@@H](N3C[C@@](CCC4=O)([H])N4CC3)CC1)N([C@@H](C5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5)C)C.O=C(O)/C=C\C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (40.28 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3428 mL 6.7141 mL 13.4282 mL
5 mM 0.2686 mL 1.3428 mL 2.6856 mL
10 mM 0.1343 mL 0.6714 mL 1.3428 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 5 mg/mL (6.71 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (6.71 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (6.71 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
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Orvepitant maleate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Orvepitant579475-24-4GW823296GW 823296GW-823296Neurokinin ReceptorNK receptorTachykinin receptorCRCsafewell-toleratedsubstance-Plong-lastingantidepressantCNSpharmacokineticsdepressivedisorderInhibitorinhibitorinhibit

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