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

Orvepitant maleate (Synonyms: GW823296 maleate)

Cat. No.: HY-122347A
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

Size Price Stock
5 mg USD 200 Ask For Quote & Lead Time
10 mg USD 350 Ask For Quote & Lead Time
25 mg USD 700 Ask For Quote & Lead Time
50 mg USD 1100 Ask For Quote & Lead Time
100 mg USD 1650 Ask For Quote & Lead Time

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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

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].

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

Formula

C35H39F7N4O6

CAS No.
SMILES

O=C(N1[[email protected]@H](C2=CC=C(F)C=C2C)C[[email protected]@H](N3C[[email protected]@](CCC4=O)([H])N4CC3)CC1)N([[email protected]@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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Orvepitant maleate
Cat. No.:
HY-122347A
Quantity:
MCE Japan Authorized Agent: