Capromorelin tartrate
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MedKoo CAT#: 326824

CAS#: 193273-69-7 (tartrate)

Description: Capromorelin, 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.

Chemical Structure

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Capromorelin tartrate
CAS# 193273-69-7 (tartrate)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 326824
Name: Capromorelin tartrate
CAS#: 193273-69-7 (tartrate)
Chemical Formula: C32H41N5O10
Exact Mass: 655.29
Molecular Weight: 655.705
Elemental Analysis: C, 58.62; H, 6.30; N, 10.68; O, 24.40

Price and Availability

Size Price Availability Quantity
100mg USD 1450
200mg USD 1950
500mg USD 2950
1g USD 3850 2 Weeks
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Related CAS #: 193273-66-4 (free base)   193273-69-7 (tartrate)    

Synonym: CP-424,391; CP 424,391; CP424,391; CP-424391; CP 424391; CP424391; CP-424,391-18; Capromorelin tartrate.

IUPAC/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

InChi Key: MJGRJCMGMFLOET-MYPSAZMDSA-N

InChi Code: 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

SMILES Code: CC(C)(N)C(N[C@@H](C(N(C[C@]12CC3=CC=CC=C3)CCC1=NN(C)C2=O)=O)COCC4=CC=CC=C4)=O.O[C@H]([C@H](C(O)=O)O)C(O)=O

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Related CAS# CAS#193273-69-7 (Capromorelin tartrate) CAS#193273-66-4 (Capromorelin free base)

Product Data:
Product Data
Instruction:
View handling instruction
Biological target:
In vitro activity:
In vivo activity: The in vivo GH activities of the PP dipeptide analogues were measured in an anesthesized rat model following iv administration. Capromorelin and compounds 5b and 5c stimulated GH secretion after a single 1 mg/kg dose, though the mean GH peak heights for capromorelin and 5c were significantly higher than the mean GH peak height for 5b (data not shown). Capromorelin and 5c showed similar dose–response relationships in the model, with ED50 values less than 0.05 mg/kg iv. The weaker in vivo activity of the N-ethyl PP derivative 5b was attributed to its increased lipophilicity, which could have reduced the amount of unbound drug in the plasma compartment capable of interacting with the GHS-R1a. Reference: Bioorg Med Chem. 2003 Feb 20;11(4):581-90. https://linkinghub.elsevier.com/retrieve/pii/S0968089602004339

Preparing Stock Solutions

The following data is based on the product molecular weight 655.71 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol: 1. Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Cook ER, DiBrino JN, Campeta AM, DeNinno SL, Chidsey-Frink KL, Hada WA, Inthavongsay J, Mangano FM, Mullins MA, Nickerson DF, Ng O, Pirie CM, Ragan JA, Rose CR, Tess DA, Wright AS, Yu L, Zawistoski MP, DaSilva-Jardine PA, Wilson TC, Thompson DD. Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin. Bioorg Med Chem. 2003 Feb 20;11(4):581-90. doi: 10.1016/s0968-0896(02)00433-9. PMID: 12538023. 2. Zollers B, Rhodes L, Heinen E. 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. doi: 10.1186/s12917-016-0925-z. PMID: 28056951; PMCID: PMC5217407.

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1: Broad J, Callaghan B, Sanger GJ, Brock JA, Furness JB. Analysis of the ghrelin receptor-independent vascular actions of ulimorelin. Eur J Pharmacol. 2015 Apr 5;752:34-9. doi: 10.1016/j.ejphar.2015.02.005. Epub 2015 Feb 14. PubMed PMID: 25687251.

2: Pustovit RV, Furness JB, Rivera LR. A ghrelin receptor agonist is an effective colokinetic in rats with diet-induced constipation. Neurogastroenterol Motil. 2015 May;27(5):610-7. doi: 10.1111/nmo.12517. Epub 2015 Jan 19. PubMed PMID: 25616061.

3: Ellis AG, Zeglinski PT, Brown DJ, Frauman AG, Millard M, Furness JB. Pharmacokinetics of the ghrelin agonist capromorelin in a single ascending dose Phase-I safety trial in spinal cord-injured and able-bodied volunteers. Spinal Cord. 2015 Feb;53(2):103-8. doi: 10.1038/sc.2014.218. Epub 2014 Dec 2. PubMed PMID: 25448190.

4: Docanto MM, Yang F, Callaghan B, Au CC, Ragavan R, Wang X, Furness JB, Andrews ZB, Brown KA. Ghrelin and des-acyl ghrelin inhibit aromatase expression and activity in human adipose stromal cells: suppression of cAMP as a possible mechanism. Breast Cancer Res Treat. 2014 Aug;147(1):193-201. doi: 10.1007/s10549-014-3060-1. Epub 2014 Jul 24. PubMed PMID: 25056185.

5: Callaghan B, Kosari S, Pustovit RV, Sartor DM, Ferens D, Ban K, Baell J, Nguyen TV, Rivera LR, Brock JA, Furness JB. Hypotensive effects of ghrelin receptor agonists mediated through a novel receptor. Br J Pharmacol. 2014 Mar;171(5):1275-86. doi: 10.1111/bph.12527. PubMed PMID: 24670149; PubMed Central PMCID: PMC3952804.

6: Callaghan B, Hunne B, Hirayama H, Sartor DM, Nguyen TV, Abogadie FC, Ferens D, McIntyre P, Ban K, Baell J, Furness JB, Brock JA. Sites of action of ghrelin receptor ligands in cardiovascular control. Am J Physiol Heart Circ Physiol. 2012 Oct 15;303(8):H1011-21. doi: 10.1152/ajpheart.00418.2012. Epub 2012 Aug 10. PubMed PMID: 22886413.

7: Portelli J, Thielemans L, Ver Donck L, Loyens E, Coppens J, Aourz N, Aerssens J, Vermoesen K, Clinckers R, Schallier A, Michotte Y, Moechars D, Collingridge GL, Bortolotto ZA, Smolders I. Inactivation of the constitutively active ghrelin receptor attenuates limbic seizure activity in rodents. Neurotherapeutics. 2012 Jul;9(3):658-72. doi: 10.1007/s13311-012-0125-x. PubMed PMID: 22669710; PubMed Central PMCID: PMC3441926.

8: Ferens DM, Habgood MD, Saunders NR, Tan YH, Brown DJ, Brock JA, Furness JB. Stimulation of defecation in spinal cord-injured rats by a centrally acting ghrelin receptor agonist. Spinal Cord. 2011 Oct;49(10):1036-41. doi: 10.1038/sc.2011.60. Epub 2011 May 31. PubMed PMID: 21625243.

9: Ferens DM, Yin L, Ohashi-Doi K, Habgood M, Bron R, Brock JA, Gale JD, Furness JB. Evidence for functional ghrelin receptors on parasympathetic preganglionic neurons of micturition control pathways in the rat. Clin Exp Pharmacol Physiol. 2010 Sep;37(9):926-32. doi: 10.1111/j.1440-1681.2010.05409.x. Epub 2010 May 24. PubMed PMID: 20497419.

10: Lacheretz R, Pardo DG, Cossy J. Daucus carota mediated-reduction of cyclic 3-oxo-amines. Org Lett. 2009 Mar 19;11(6):1245-8. doi: 10.1021/ol8029214. PubMed PMID: 19215083.

11: White HK, Petrie CD, Landschulz W, MacLean D, Taylor A, Lyles K, Wei JY, Hoffman AR, Salvatori R, Ettinger MP, Morey MC, Blackman MR, Merriam GR; Capromorelin Study Group. Effects of an oral growth hormone secretagogue in older adults. J Clin Endocrinol Metab. 2009 Apr;94(4):1198-206. doi: 10.1210/jc.2008-0632. Epub 2009 Jan 27. PubMed PMID: 19174493.

12: Hersch EC, Merriam GR. Growth hormone (GH)-releasing hormone and GH secretagogues in normal aging: Fountain of Youth or Pool of Tantalus? Clin Interv Aging. 2008;3(1):121-9. Review. PubMed PMID: 18488883; PubMed Central PMCID: PMC2544358.

13: Thompson DD. Aging and sarcopenia. J Musculoskelet Neuronal Interact. 2007 Oct-Dec;7(4):344-5. PubMed PMID: 18094505.

14: Lanz TA, Salatto CT, Semproni AR, Marconi M, Brown TM, Richter KE, Schmidt K, Nelson FR, Schachter JB. Peripheral elevation of IGF-1 fails to alter Abeta clearance in multiple in vivo models. Biochem Pharmacol. 2008 Mar 1;75(5):1093-103. Epub 2007 Nov 12. PubMed PMID: 18076866.

15: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Apr;29(3):231-45. PubMed PMID: 17520107.

16: Sutton SC, Evans LA, Fortner JH, McCarthy JM, Sweeney K. Dog colonoscopy model for predicting human colon absorption. Pharm Res. 2006 Jul;23(7):1554-63. Epub 2006 Jun 21. PubMed PMID: 16783662.

17: Kitazawa T, De Smet B, Verbeke K, Depoortere I, Peeters TL. Gastric motor effects of peptide and non-peptide ghrelin agonists in mice in vivo and in vitro. Gut. 2005 Aug;54(8):1078-84. Epub 2005 Apr 20. PubMed PMID: 15843418; PubMed Central PMCID: PMC1774892.

18: Khojasteh-Bakht SC, O'donnell JP, Fouda HG, Potchoiba MJ. Metabolism, pharmacokinetics, tissue distribution, and excretion of [14C]CP-424391 in rats. Drug Metab Dispos. 2005 Jan;33(1):190-9. Epub 2004 Oct 14. PubMed PMID: 15486077.

19: Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Cook ER, DiBrino JN, Campeta AM, DeNinno SL, Chidsey-Frink KL, Hada WA, Inthavongsay J, Mangano FM, Mullins MA, Nickerson DF, Ng O, Pirie CM, Ragan JA, Rose CR, Tess DA, Wright AS, Yu L, Zawistoski MP, DaSilva-Jardine PA, Wilson TC, Thompson DD. Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin. Bioorg Med Chem. 2003 Feb 20;11(4):581-90. PubMed PMID: 12538023.

20: Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Murray MC, Cook ER, DiBrino JN, DeNinno SL, Chidsey-Frink KL, Hada WA, Inthavongsay J, Lewis SK, Mangano FM, Mullins MA, Nickerson DF, Ng O, Pirie CM, Ragan JA, Rose CR, Tess DA, Wright AS, Yu L, Zawistoski MP, Pettersen JC, DaSilva-Jardine PA, Wilson TC, Thompson DD. Discovery and biological characterization of capromorelin analogues with extended half-lives. Bioorg Med Chem Lett. 2002 Nov 18;12(22):3279-82. PubMed PMID: 12392732.