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AS-1517499 — Datasheet

CAT. NO. DC11420

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ParameterValue
Chemical Name4-(Benzylamino)-2-((3-chloro-4-hydroxyphenethyl)amino)pyrimidine-5-carboxamide
CAS No.919486-40-1
Synonyms4-(Benzylamino)-2-((3-chloro-4-hydroxyphenethyl)amino)pyrimidine-5-carboxamide;4-(benzylamino)-2-[2-(3-chloro-4-hydroxyphenyl)ethylamino]pyrimidine-5-carboxamide;5-Pyrimidinecarboxamide, 2-[[2-(3-chloro-4-hydroxyphenyl)ethyl]amino]-4-[(phenylmethyl)amino]-;AS 1517499;AS-1517499;2-[[2-(3-Chloro-4-hydroxyphenyl)ethyl]amino]-4-[(phenylmethyl)amino]-5-pyrimidinecarboxamide;4-(Benzylamino)-2-{[2-(3-chloro-4-hydroxyphenyl)ethyl]amino}pyrimidine-5-carboxamide;AS1517499;2H31HOT08T;OZRMEKAUZBKTTC-UHFFFAOYSA-N;HMS3740O03;BCP13796;BDBM50197554;s8685;AS-
FormulaC20H20ClN5O2
M.Wt397.8581
SMILESClC1=C(C([H])=C([H])C(=C1[H])C([H])([H])C([H])([H])N([H])C1=NC([H])=C(C(N([H])[H])=O)C(=N1)N([H])C([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])O[H]
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

AS1517499 is a potent STAT6 inhibitor with an IC50 of 21 nM.

In Vitro

AS1517499 shows potent STAT6 inhibition with an IC50 value of 21 nM, and also inhibits IL-4-induced Th2 differentiation of mouse spleen T cells with an IC50 value of 2.3 nM and without influencing T-helper cell 1 (Th1) differentiation induced by IL-12. AS1517499 selectively inhibits Th2 differentiation without affecting Th1 differentiation[1]. In cultured human BSM cells, IL-13 (100 ng/mL) causes a phosphorylation of STAT6 and an up-regulation of RhoA, a monomeric GTPase responsible for Ca2+ sensitization of smooth muscle contraction: both events are inhibited by co-incubation with AS1517499 (100 nM)[2].

In Vivo

In BALB/c mice that are actively sensitized and repeatedly challenged with ovalbumin antigen, an increased IL-13 level in bronchoalveolar lavage fluids and a phosphorylation of STAT6 in bronchial tissues are observed after the last antigen challenge. These mice have an augmented BSM contractility to acetylcholine together with an up-regulation of RhoA in bronchial tissues. Intraperitoneal injections of AS1517499 (10 mg/kg) 1 hour before each ovalbumin exposure inhibits both the antigen-induced up-regulation of RhoA and BSM hyperresponsiveness, almost completely[2].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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