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130408-77-4

130408-77-4 structure
130408-77-4 structure
  • Name: A-71623 TFA
  • Chemical Name: Boc-Trp-Lys(Tac)-Asp-N(Me)Phe-NH2
  • CAS Number: 130408-77-4
  • Molecular Formula: C44H56N8O9
  • Molecular Weight: 840.96
  • Catalog: Signaling Pathways GPCR/G Protein Cholecystokinin Receptor
  • Create Date: 2016-11-26 06:15:08
  • Modify Date: 2024-01-05 17:27:45
  • A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively[1].
Name Boc-Trp-Lys(Tac)-Asp-N(Me)Phe-NH2
Synonyms Boc-Trp-His-OMe
Description A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively[1].
Related Catalog
Target

IC50: 3.7 nM (CCKA receptor in radioligand binding assays)[1]
In Vitro In guinea pig gastric glands, the affinities of A-71623 for the cholecystokinin (CCK)-B/gastrin receptor were 11 μM[1].
In Vivo A71623 (A-63387; i.c.v., but not i.p., injections) reduces food intakes and suppresses intakes of a liquid diet in both deprived and sated rats[2]. A71623 dampens Purkinje neuron pathology and associates deficits in motor performance in Pcp2-ATXN1[30Q]D776;Cck-/- and Pcp2-AXTN1[82Q] mice[3]. A71623 improves motor performance of Pcp2-ATXN2[127Q] SCA2 mice[3]. Animal Model: Adult male, Sprague-Dawley rats[2] Dosage: 5 μL Administration: Intracerebroventricular (i.c.v) administration, A-71623 was infused using a 28 gauge injection cannula in a volume of 5uL over 60 s Result: Reduced food intakes and suppressed intakes of a liquid diet. Animal Model: ATXN1[30Q]-D776, ATXN1[82Q]-D776, ATXN2[127Q], and WT/FVB/NJ mice [3] Dosage: 0.02 mg/kg/day Administration: Osmotic minipumps containing either A71623 (0.02mg/kg/day) were implanted intraperitoneally (i.p.) Result: Treatment dampened Purkinje neuron pathology in ATXN1[30Q]D776;Cck-/- mice and ATXN1[82Q] mice. Improved motor performance in ATXN2[127Q] mice.
References

[1]. C W Lin, et al. Characterization of two novel cholecystokinin tetrapeptide (30-33) analogues, A-71623 and A-70874, that exhibit high potency and selectivity for cholecystokinin-A receptors. Mol Pharmacol. 1991 Mar;39(3):346-51.

[2]. K E Asin, et al. Effects of selective CCK receptor agonists on food intake after central or peripheral administration in rats. Brain Res. 1992 Jan 31;571(1):169-74.

[3]. Emily A.L. Wozniak, et al. Cholecystokinin 1 Receptor (Cck1R) Activates mTORC1 signaling and is Protective to Purkinje cells in SCA Mice.  bioRxiv. February 17, 2021.
Molecular Formula C44H56N8O9
Molecular Weight 840.96
Exact Mass 840.41700
PSA 254.15000
LogP 6.24030
Storage condition -20°C
Precursor  1

DownStream  0


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title: CAS No. 130408-77-4 | Chemsrc address: https://m.chemsrc.com/en/baike/671961.html

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