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145455-35-2

145455-35-2 structure
145455-35-2 structure
  • Name: L-692,585
  • Chemical Name: 3-[[(2R)-2-hydroxypropyl]amino]-3-methyl-N-[(3R)-2-oxo-1-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-4,5-dihydro-3H-1-benzazepin-3-yl]butanamide
  • CAS Number: 145455-35-2
  • Molecular Formula: C32H37N7O3
  • Molecular Weight: 567.68100
  • Catalog: Signaling Pathways GPCR/G Protein GHSR
  • Create Date: 2017-12-24 22:06:47
  • Modify Date: 2024-01-08 20:20:55
  • L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a Ki of 0.8 nM. L-692585 acts directly on somatotropes causing GH release[1][2].
Name 3-[[(2R)-2-hydroxypropyl]amino]-3-methyl-N-[(3R)-2-oxo-1-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-4,5-dihydro-3H-1-benzazepin-3-yl]butanamide
Synonyms hms3268f14
l-692,585
Description L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a Ki of 0.8 nM. L-692585 acts directly on somatotropes causing GH release[1][2].
Related Catalog
Target

Ki: 0.8 nM (GHS-R1a)[1]

In Vitro L-692585 (10 µM; 2 min) produces a prompt transient increase in [Ca2+]i, following by the sustained decline to a plateau above the basal level in GH cells[2]. L-692585 (0.01-10 µM; 2 min) induces release of growth hormone (GH) in a dose-dependent manner from isolated porcine somatotropes[2]. L-692585 (100 nM) significantly increases the number and size of plaques, and it also causes a significant increase in total secretion index (TSI) [2].
In Vivo L-692585 (0.01-0.1 mg/kg; i.v. once daily for 2 weeks) increases peak plasma GH levels and total GH release[3]. L-692585 (0.005-0.1 mg/kg; a single i.v.) significantly increases peak GH concentrations 4.3-fold at a dose of 0.005 mg/kg, 7-fold at a dose of 0.02 mg/kg, and 21-fold at a dose of 0.10 mg/kg in vivo[3]. Animal Model: Beagles (1-1.5 years old ; weighting 8.5-16.0 kg)[3] Dosage: 0.01, 0.1 mg/kg Administration: I.v. once daily for 2 weeks Result: Increased the peak plasma GH levels and total GH release on days 1, 8 and 15 in a dose-dependent manner, and no desensitization was evident.
References

[1]. Smith RG, et, al. Peptidomimetic regulation of growth hormone secretion. Endocr Rev. 1997 Oct; 18(5): 621-45.

[2]. Glavaski-Joksimovic A, et, al. Mechanism of action of the growth hormone secretagogue, L-692,585, on isolated porcine somatotropes. J Endocrinol. 2002 Dec; 175(3): 625-36.

[3]. Jacks T, et, al. Effects of acute and repeated intravenous administration of L-692,585, a novel non-peptidyl growth hormone secretagogue, on plasma growth hormone, IGF-1, ACTH, cortisol, prolactin, insulin, and thyroxine levels in beagles. J Endocrinol. 1994 Nov; 143(2): 399-406.
Density 1.31g/cm3
Molecular Formula C32H37N7O3
Molecular Weight 567.68100
Exact Mass 567.29600
PSA 136.13000
LogP 4.48380
Index of Refraction 1.66
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