A 71623
A 71623 Basic information
- Product Name:
- A 71623
- Synonyms:
-
- N-[(1,1-DIMETHYLETHOXY)CARBONYL]-L-TRYPTOPHYL-N6-[[(2-METHYLPHENYL)AMINO]CARBONYL]-L-LYSYL-L-ALPHA-ASPARTYL-NA-METHYL-L-PHENYLALANINAMIDE
- N-Boc-L-Trp-[(2S)-2-Amino*-6-[3-(2-methylphenyl)ureido]hexanoyl]-L-Asp-N-methyl-L-Phe-NH2
- N-[(1,1-Dimethylethoxy)carbonyl]-L-tryptophyl-N6-[[(2-methylphenyl)amino]carbonyl]-L-lysyl-L-α-aspartyl-Nα-methyl-L-phenylalaninamide
- A 71623
- L-Phenylalaninamide, N-[(1,1-dimethylethoxy)carbonyl]-L-tryptophyl-N6-[[(2-methylphenyl)amino]carbonyl]-L-lysyl-L-α-aspartyl-Nα-methyl-
- A-71623 TFA
- CAS:
- 130408-77-4
- MF:
- C44H56N8O9
- MW:
- 840.96
- Mol File:
- 130408-77-4.mol
A 71623 Chemical Properties
- storage temp.
- Desiccate at -20°C
- solubility
- Soluble to 1 mg/ml in 20mM PBS buffer
- form
- solid
- color
- White
A 71623 Usage And Synthesis
Uses
A-71623 is a potent CCK agonist with 1200-fold selectivity over the CCK2 receptor.
Biological Activity
Potent CCK 1 agonist (IC 50 = 3.7 nM) with 1200-fold selectivity over the CCK 2 receptor. Suppresses food intake following central or peripheral administration.
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. |
IC 50
CCKAR
storage
Store at -20°C
References
[1]. gracey dj, bell r, king dj. differential effects of the ccka receptor ligands pd-140,548 and a-71623 on latent inhibition in the rat. progress in neuro-psychopharmacology and biological psychiatry, 2002, 26(3): 497-504.
[2]. lin cw, shiosaki k, miller tr, 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. molecular pharmacology, 1991, 39(3): 346-351.
[3]. kaufmann r, lindschau c, scho t, et al. type b cholecystokinin receptors on rat glioma c6 cells. binding studies and measurement of intracellular calcium mobilization. brain research, 1994, 639(1): 109-114.
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