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Cat. No.: HY-153095A

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PF-6870961 hydrochloride

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

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

CAS No.: 2857112-07-1
Formula: C₂₉H₃₃ClN₆O₂S
Molecular Weight:565.13

Storage:

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

Data Sheet (273 KB)

PF-6870961 hydrochloride Chemical Structure

CAS No.: 2857112-07-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All GHSR Isoforms :

GHSR1a

In Vivo

PF-6870961 hydrochloride (40 mg/kg; i.p.) suppresses food intake in both satiated and fasted rats^[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.

Chemical Information

CAS No. 2857112-07-1
Molecular Weight 565.13
Formula C₂₉H₃₃ClN₆O₂S
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.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Deschaine SL, et al. Initial pharmacological characterization of a major hydroxy metabolite of PF-5190457: inverse agonist activity of PF-6870961 at the ghrelin receptor. J Pharmacol Exp Ther. 2023 Jan 11:JPET-AR-2022-001393. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- In Vivo
Chemical Information
Purity & Documentation
References

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PF-6870961 hydrochloride

All GHSR Isoforms