CAPROMORELIN

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C28H35N5O4
Molecular Weight	505.6086
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CN1N=C2CCN(C[C@@]2(CC3=CC=CC=C3)C1=O)C(=O)[C@@H](COCC4=CC=CC=C4)NC(=O)C(C)(C)N

InChI

InChIKey=KVLLHLWBPNCVNR-SKCUWOTOSA-N

InChI=1S/C28H35N5O4/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/h4-13,22H,14-19,29H2,1-3H3,(H,30,35)/t22-,28-/m1/s1

HIDE SMILES / InChI

Description

Capromorelin is a potent ghrelin receptor agonist. Capromorelin is indicated for appetite stimulation in dogs. Plasma insulin-like growth factor-I (IGF-I) was elevated progressively over a 5-d course of daily oral dosing in dogs. In healthy older adults at risk for functional decline, administration of the capromorelin may improve body composition and physical function. Adverse events included fatigue, insomnia, and small increases in fasting glucose, glycosylated hemoglobin, and indices of insulin resistance.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Ghrelin receptor 15	Agonist 2,752		7.0 nM [Ki]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Inappetence 2	Palliative		Approved 8,583	ENTYCE
Aging 4	Palliative		Phase II 1,147	Unknown

C_max

Value	Dose	Analyte	Population
28.1 ng/mL	20 mg single, oral	CAPROMORELIN plasma	Homo sapiens
90.5 ng/mL	50 mg single, oral	CAPROMORELIN plasma	Homo sapiens
187.1 ng/mL	100 mg single, oral	CAPROMORELIN plasma	Homo sapiens
33.9 ng/mL	20 mg single, oral	CAPROMORELIN plasma	Homo sapiens
71.2 ng/mL	50 mg single, oral	CAPROMORELIN plasma	Homo sapiens
206.5 ng/mL	100 mg single, oral	CAPROMORELIN plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
97.9 ng × h/mL	20 mg single, oral	CAPROMORELIN plasma	Homo sapiens
254.6 ng × h/mL	50 mg single, oral	CAPROMORELIN plasma	Homo sapiens
527.8 ng × h/mL	100 mg single, oral	CAPROMORELIN plasma	Homo sapiens
135.3 ng × h/mL	20 mg single, oral	CAPROMORELIN plasma	Homo sapiens
346 ng × h/mL	50 mg single, oral	CAPROMORELIN plasma	Homo sapiens
798.9 ng × h/mL	100 mg single, oral	CAPROMORELIN plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
2.75 h	20 mg single, oral	CAPROMORELIN plasma	Homo sapiens
2.54 h	50 mg single, oral	CAPROMORELIN plasma	Homo sapiens
2.56 h	100 mg single, oral	CAPROMORELIN plasma	Homo sapiens
3.02 h	20 mg single, oral	CAPROMORELIN plasma	Homo sapiens
3.1 h	50 mg single, oral	CAPROMORELIN plasma	Homo sapiens
2.91 h	100 mg single, oral	CAPROMORELIN plasma	Homo sapiens

Doses

Doses

Show entries

Dose	Population	Adverse events
100 mg single, oral Highest studied dose	unhealthy, ADULT

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PubMed

Show entries

Title	Date	PubMed
The prokinetic face of ghrelin.	2010	20721347
Evidence for functional ghrelin receptors on parasympathetic preganglionic neurons of micturition control pathways in the rat.	2010 Sep	20497419
Smaller cardiac cell size and reduced extra-cellular collagen might be beneficial for hearts of Ames dwarf mice.	2010 Sep 1	20827400

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Patents

Sample Use Guides

In Vivo Use Guide

Dog: 3 mg/kg body weight once daily

Route of Administration: Oral

In Vitro Use Guide

In rat pituitary cell cultures, Capromorelin stimulated growth hormone release with an EC50 = 3 nM.

Show entries

Name

Type

Language

CP-424,391

Preferred Name

English

CAPROMORELIN

Official Name

English

CAPIMORELIN

Common Name

English

PROPANAMIDE, 2-AMINO-N-(2-(2,3,3A,4,6,7-HEXAHYDRO-2-METHYL-3-OXO-3A-(PHENYLMETHYL)-5H-PYRAZOLO(4,3-C)PYRIDIN-5-YL)-2-OXO-1-((PHENYLMETHOXY)METHYL)ETHYL)-2-METHYL-, (R-(R*,R*))-

Common Name

English

CP-424391

Code

English

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Show entries

Classification Tree

Code System

Code

PART 520 ORAL DOSAGE FORM NEW ANIMAL DRUGS

CFR

21 CFR 520.292

Therapeutic Hormone

NCI_THESAURUS

C76358

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Code System

Code

Type

Description

CAS

329327-00-6

SUPERSEDED

MERCK INDEX

m11965

PRIMARY

EPA CompTox

DTXSID5057886

PRIMARY

DAILYMED

0MQ44VUN84

PRIMARY

RXCUI

1986787

PRIMARY

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ACTIVE MOIETY


					0MQ44VUN84

CAPROMORELIN

SALT/SOLVATE (PARENT)


					4150VMF5EP

CAPROMORELIN TARTRATE

SMILES

InChI

CNS Activity

Originator

Approval Year

Targets

Conditions

Cmax

AUC

T1/2

Doses

PubMed

Patents

Sample Use Guides

C_max

T_1/2