Capromorelin Tartrate

Capromorelin Tartrate, also known as CP-424, 391, is a growth hormone secretagogue and ghrelin mimetic ( hGHS-R1a K(i)=7 nM, rat pituicyte EC(50)=3 nM). Initial studies have shown the drug to directly raise insulin growth factor 1 (IGF-1) and growth hormone levels. Capromorelin showed enhanced intestinal absorption in rodent models and exhibited superior pharmacokinetic properties, including high bioavailabilities in two animal species [F(rat)=65%, F(dog)=44%]. This short-duration GHS was orally active in canine models and was selected as a development candidate for the treatment of musculoskeletal frailty in elderly adults.

Product information

CAS Number: 193273-69-7

Molecular Weight: 655.70

Formula: C32H41N5O10

Synonym:

CP-424, 391

CP 424, 391

CP424, 391

CP-424,391

CP 424,391

CP424,391

CP-424391

CP 424391

CP424391

CP-424,391-18

Capromorelin tartrate.

Chemical Name: 2-amino-N-((R)-1-((R)-3a-benzyl-2-methyl-3-oxo-2, 3, 3a, 4, 6, 7-hexahydro-5H-pyrazolo[4, 3-c]pyridin-5-yl)-3-(benzyloxy)-1-oxopropan-2-yl)-2-methylpropanamide (2R, 3R)-2, 3-dihydroxysuccinate

Smiles: CC(C)(N)C(=O)N[C@H](COCC1C=CC=CC=1)C(=O)N1C[C@]2(CC3C=CC=CC=3)C(CC1)=NN(C)C2=O.OC(=O)[C@H](O)[C@@H](O)C(O)=O

InChiKey: MJGRJCMGMFLOET-MYPSAZMDSA-N

InChi: InChI=1S/C28H35N5O4.C4H6O6/c1-27(2,29)25(35)30-22(18-37-17-21-12-8-5-9-13-21)24(34)33-15-14-23-28(19-33,26(36)32(3)31-23)16-20-10-6-4-7-11-20;5-1(3(7)8)2(6)4(9)10/h4-13,22H,14-19,29H2,1-3H3,(H,30,35);1-2,5-6H,(H,7,8)(H,9,10)/t22-,28-;1-,2-/m11/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 100 mg/mL (152.51 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Capromorelin stimulates GH release in rat pituitary cell cultures with EC50 of 3 nM.

In Vivo:

Dogs receiving capromorelin (30 mg/mL) have food consumption that is significantly greater than dogs treated with placebo. All dogs in the capromorelin group gain weight by 0.52 kg, more than that of placebo grou. Capromorelin shows enhanced intestinal absorption in rodent models and exhibits superior pharmacokinetic properties, including high bioavailabilities in two animal species [F(rat)=65%, F(dog)=44%. Capromorelin stimulates GH release in anesthesized rat model, with ED50 of 0.05 mg/kg iv.

References:

1. Zollers B, et al. Capromorelin oral solution (ENTYCE?) increases food consumption and body weight when administered for 4 consecutive days to healthy adult Beagle dogs in a randomized, masked, placebo controlled study. BMC Vet Res. 2017 Jan 5;13(1):10.
2. Carpino PA, et al. Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin. Bioorg Med Chem. 2003 Feb 20;11(4):581-90.

Products are for research use only. Not for human use.