PHENOLPHTHALEIN DIPHOSPHATE TETRASODIUM

PHENOLPHTHALEIN DIPHOSPHATE TETRASODIUM Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Psora 4 is an inhibitor of voltage-gated potassium channels (K_v1.3; EC₅₀ = 3 nM). It is selective for K_v1.3 over K_v1.1, K_v1.2, K_v1.4, K_v1.7, and K_v3.1 channels (EC₅₀s = 62, 49, 202, 100, and 1,500 nM, respectively) but does inhibit the K_v1.5 channel (EC₅₀ = 7.7 nM). Psora 4 selectively binds to the C-type inactivated state of the K_v1.3 channel and inhibits potassium current in a use-dependent manner. It has immunosuppressive activity, inhibiting proliferation of human and rat myelin-specific effector memory T cells in vitro (TEM cells; EC₅₀s = 25 and 60 nM, respectively).

Verwenden

Psora-4 is the most potent small-molecule Kv1.3 blocker known. Psora-4 and other Kv1.3 blockers may be useful as immunomodulators for the therapy of autoimmune disorders.

Biochem/physiol Actions

The lymphocyte potassium channel Kv1.3 is regarded as a new target for immunosuppression. Psora-4 is the most potent small-molecule Kv1.3 blocker known. It blocked Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50 value of 3 nM, by preferentially binding to the C-type inactivated state of the channel. It exhibited 17- to 70-fold selectivity for Kv1.3 over closely related Kv1-family channels (Kv1.1, Kv1.2, Kv1.4, and Kv1.7) with the exception of Kv1.5 (EC50, 7.7 nM) and showed no effect on human ether-a-go-go-related channel, Kv3.1, the calcium-activated K+ channels (IKCa1, SK1-SK3, and BKCa), or the neuronal NaV1.2 channel. In a test of in vivo toxicity in rats, Psora-4 did not display any signs of acute toxicity after five daily subcutaneous injections at 33 mg/kg body weight. Psora-4 selectively suppressed the proliferation of human and rat myelin-specific effector memory T cells with EC50 values of 25 and 60 nM, respectively, without persistently suppressing peripheral blood naive and central memory T cells. Because autoantigen-specific effector memory T cells contribute to the pathogenesis of T cell-mediated autoimmune diseases such as multiple sclerosis, Psora-4 and other Kv1.3 blockers may be useful as immunomodulators for the therapy of autoimmune disord.

PHENOLPHTHALEIN DIPHOSPHATE TETRASODIUM Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

PHENOLPHTHALEIN DIPHOSPHATE TETRASODIUM Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58
J & K SCIENTIFIC LTD.	010-82848833 400-666-7788	jkinfo@jkchemical.com	China	94838	76
Chemsky (shanghai) International Co.,Ltd	021-50135380	shchemsky@sina.com	China	15421	60
Sigma-Aldrich	021-61415566 800-8193336	orderCN@merckgroup.com	China	51471	80
EMMX Biotechnology LLC	888-539-0666	info@emmx.com	United States	8449	60
Shenzhen Polymeri Biochemical Technology Co., Ltd.	+86-400-002-6226 13028896684	sales@rrkchem.com	China	55894	58
BOC Sciences	--	info@bocsci.com	USA	0	65
DC Chemicals	021-58447131 13564518121	sales@dcchemicals.com	China	9414	58
ChemeGen(Shanghai) Biotechnology Co.,Ltd.	18818260767	sales@chemegen.com	China	11289	58
MedBioPharmaceutical Technology Inc	021-69568360 18916172912	order@med-bio.cn	China	8141	58

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