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Cat. No.: HY-153095

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PF-6870961

PF-6870961 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 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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CAS No.: 2857112-06-0
화학식: C₂₉H₃₂N₆O₂S
분자량:528.67

보관:

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

Data Sheet (272 KB)

PF-6870961 Chemical Structure

CAS No.: 2857112-06-0

Amount: USD 0.00

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Use of MCE Products

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

Biological Activity

제품 설명

All GHSR Isoforms :

GHSR1a

In Vivo

PF-6870961 (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. 2857112-06-0
분자량 528.67
화학식 C₂₉H₃₂N₆O₂S
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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 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]

Calculators

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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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MOQ

Minimum order quantity

100 mg

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