2. GPCR/G Protein
  3. GHSR
  4. PF-6870961

PF-6870961 is an inverse agonist of GHSR1a with Ki values of 73.6 nM (human GHSR), 239 nM (rat GHSR), and 217 nM (dog GHSR), respectively. PF-6870961 inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM.

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PF-6870961 Chemical Structure

PF-6870961 Chemical Structure

CAS No. : 2857112-06-0

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PF-6870961 Related Antibodies

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Description

PF-6870961 is an inverse agonist of GHSR1a with Ki values of 73.6 nM (human GHSR), 239 nM (rat GHSR), and 217 nM (dog GHSR), respectively. PF-6870961 inhibits the constitutive GHSR1a-induced IP accumulation with an IC50 value of 300 nM. PF-6870961 also inhibits constitutive GHSR1a β-arrestin mobilization with an IC50 value of 1.10 nM[1].

In Vivo

PF-6870961 (40 mg/kg；腹腔注射) 抑制饱食和禁食大鼠的食物摄入[1]。

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

Animal Model: Satiated and fasted rats model[1]
Dosage: 2.5 mg/kg, 10 mg/kg, and 40 mg/kg
Administration: Intraperitoneal injection
Result: Significantly reduced food intake at 40 mg/kg.
Molecular Weight

528.67

Formula

C29H32N6O2S
CAS No.
SMILES

CC1=CN(C(S1)=N2)C=C2CC(N3CCC4(CC3)CN([C@H]5C6=CC=C(C7=NC(O)=NC(C)=C7)C=C6CC5)C4)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PF-6870961 Related Classifications

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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.

Keywords:

PF-68709612857112-06-0PF6870961PF 6870961GHSRGrowth hormone secretagogue receptorGhrelin receptorInhibitorinhibitorinhibit

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