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A-770041

SKU: orb2695751

Description

A-770041 is a selective, orally bioavailable Lck inhibitor that suppresses IL-2 production in stimulated whole blood and prevents cardiac allograft rejection. It also attenuates pulmonary fibrosis by reducing TGF-β from regulatory T cells, making it a research tool for studying immunology and fibrosis in vitro and in vivo.

Research Area

Cardiovascular Research, Signal Transduction

Images & Validation

Key Properties

CAS Number869748-10-7
MW621.73
Purity99.86%
FormulaC34H39N9O3
SMILESNC1=C2C(=NN(C2=NC=N1)[C@H]3CC[C@@H](CC3)N4CCN(C(C)=O)CC4)C5=CC(OC)=C(NC(=O)C6=CC=7C(N6C)=CC=CC7)C=C5
TargetSrc
SolubilityDMSO:20 mg/mL (32.17 mM)

Bioactivity

Target IC50
Lck:0.147 μM|Src:9.1 μM|Fyn:44.1 μM|FGR:14.1 μM
In Vivo
Recipient animals were treated with vehicle control or 2.5 to 20 mg/kg/day of A-770041 in equally. Animals were treated for 14 days, and graft viability was assessed by abdominal palpation each day. A-770041 dosed at 2.5 mg/kg/day did not lengthen graft survival time. There was a dose-dependent increase in survival with doses of 5 and 10 mg/kg/day. At doses of 10 and 20 mg/kg/day of A-770041, 100% of transplanted grafts were still beating at 14 days.
In Vitro
A-770041 selectively inhibited LCK with IC50=0.147 μM; A-770041 inhibited other SRC family kinases with SRC IC50=9.1 μM, FGR IC50=14.1 μM, and FYN IC50=44.1 μM. A-770041 dose-dependently (0-30 μM; 2 h) inhibited anti-CD3-induced IL-2 production with an EC50 = 80 nM.

Storage & Handling

Storagestore at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

rat, selective, Src, small-molecule, T cell, acute rejection, A770041, A-770041, A 770041, concanavalin A, IL-2, Lck
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Key Properties

No computed properties available.

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A-770041 (orb2695751)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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2 mg
$ 110.00
5 mg
$ 160.00
1 ml x 10 mM (in DMSO)
$ 210.00
10 mg
$ 240.00
25 mg
$ 490.00
50 mg
$ 810.00
100 mg
$ 1,230.00
200 mg
$ 1,620.00
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