Antalarmin ( HCl) is a non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist (inhibitor) with a Ki of 1 nM. Antalarmin HCl inhibits CRH-induced ACTH secretion in animal models and blocks CRH- and novelty-induced anxiety-like behaviors. Antalarmin HCl produces anti-inflammatory effects in arthritis models and inhibits stress-induced gastric ulceration associated with irritable bowel syndrome.

Physicochemical Properties

Molecular Formula	C24H35CLN4
Molecular Weight	415.01
Exact Mass	414.255
CAS #	220953-69-5
Related CAS #	Antalarmin;157284-96-3
PubChem CID	16078945
Appearance	White to light yellow solid powder
LogP	6.699
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	3
Rotatable Bond Count	6
Heavy Atom Count	29
Complexity	485
Defined Atom Stereocenter Count	0
InChi Key	CGDGXEDXEXACKQ-UHFFFAOYSA-N
InChi Code	InChI=1S/C24H34N4.ClH/c1-9-11-12-27(10-2)23-21-18(6)19(7)28(24(21)26-20(8)25-23)22-16(4)13-15(3)14-17(22)5;/h13-14H,9-12H2,1-8H3;1H
Chemical Name	N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-amine;hydrochloride
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

[1]. In vivo and in vitro characterization of antalarmin, a nonpeptide corticotropin-releasing hormone (CRH) receptor antagonist: suppression of pituitary ACTH release and peripheral inflammation. Endocrinology. 1996 Dec;137(12):5747-50. doi: 10.1210/endo.137.12.8940412. [2]. Effects of antalarmin, a CRF type 1 receptor antagonist, on anxiety-like behavior and motor activation in the rat. Brain Res. 2002 Oct 18;952(2):188-99. [3]. The impact of the nonpeptide corticotropin-releasing hormone antagonist antalarmin on behavioral and endocrine responses to stress. Endocrinology. 1999 Jan;140(1):79-86.

Solubility Data

Solubility (In Vitro)	DMF: 20 mg/mL (48.19 mM) Ethanol: 14 mg/mL (33.73 mM) DMSO: 12.5 mg/mL (30.12 mM)
Solubility (In Vivo)	Solubility in Formulation 1: 5 mg/mL (12.05 mM) in 15% Cremophor EL 85% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.4096 mL	12.0479 mL	24.0958 mL
	5 mM	0.4819 mL	2.4096 mL	4.8192 mL
	10 mM	0.2410 mL	1.2048 mL	2.4096 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.