Ruboxistaurin mesylate

小分子

鲁波西托林甲磺酸盐

UNII-6V860VW8AO | Ruboxistaurin mesylate | (18S)-18-[(dimethylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.17,14.02,6.08,13.022,27]nonacosa-1(28),2(6),7(29),8,10,12,22,24,26-nonaene-3,5-dione;methanesulfonic acid | AKOS040755510 | 13-((Dimethylamin

Ruboxistaurin mesylate

R650746-5mg

5mg

≥99%

2-8°C储存,避光,干燥

冰袋运输

Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC 50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes In Vitro Ruboxistaurin mesylate inhibits PKC isozymes with IC 50 values of 0.36, 0.0047, 0.0059, 0.30, 0.25, 0.60 and 0.052 μM for PKCα, PKCβI, PKCβII, PKCγ, PKCδ, PKCε and PKCη, respectively. Ruboxistaurin mesylate inhibits Ca calmodulin and Rat Brain PKC with IC 50 values of 6.2 and 0.32 μM, respectively. Ruboxistaurin mesylate (10 and 400 nM; 4 days) significantly suppresses glucose-induced monocyte adherence under normoglycemic (NG) conditions. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Ruboxistaurin mesylate (0.1, 1.0 and 10.0 mg/kg; oral administration, once daily for 4 weeks) decreases the increasing of leukocyte entrapment in the retinal microcirculation during the early diabetes period. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male long-evans rats with streptozotocin induced diabetesDosage: 0.1, 1.0 and 10.0 mg/kg Administration: Oral administration; 0.1, 1.0 and 10.0 mg/kg, once daily for 4 weeks Result: Significantly decreased the number of leukocytes in the retinal microcirculation of rats with streptozotocin induced diabetes. Form:Solid IC50& Target:PKC-βI 4.7 nM (IC 50 ) PKC-βII 5.9 nM (IC 50 ) PKCη 52 nM (IC 50 ) PKCδ 250 nM (IC 50 ) PKCγ 300 nM (IC 50 ) PKCα 360 nM (IC 50 ) PKCε 600 nM (IC 50 )

甲磺酸 Ruboxistaurin（LY333531）是一种口服活性、选择性和 ATP 竞争性 PKCβ 抑制剂，对 PKCβI 和 PKCβII 的 IC 50 值分别为 4.7 和 5.9 nM。甲磺酸 Ruboxistaurin 可用于研究眼部疾病、心力衰竭等疾病。

192050-59-2

C29H32N4O6S

564.65 g/mol

11577725

CN(C)C[C@@H]1CCN2C=C(C3=CC=CC=C32)C4=C(C5=CN(CCO1)C6=CC=CC=C65)C(=O)NC4=O.CS(=O)(=O)O

(18S)-18-[(dimethylamino)methyl]-17-oxa-4,14,21-triazahexacyclo[19.6.1.17,14.02,6.08,13.022,27]nonacosa-1(28),2(6),7(29),8,10,12,22,24,26-nonaene-3,5-dione;methanesulfonic acid

1S/C28H28N4O3.CH4O3S/c1-30(2)15-18-11-12-31-16-21(19-7-3-5-9-23(19)31)25-26(28(34)29-27(25)33)22-17-32(13-14-35-18)24-10-6-4-8-20(22)24;1-5(2,3)4/h3-10,16-18H,11-15H2,1-2H3,(H,29,33,34);1H3,(H,2,3,4)/t18-;/m0./s1

DUHQBKLTAVUXFF-FERBBOLQSA-N

CN(C)CC1CCN2C=C(C3=CC=CC=C32)C4=C(C5=CN(CCO1)C6=CC=CC=C65)C(=O)NC4=O.CS(=O)(=O)O

11577725

192050-59-2

DMSO : 50 mg/mL (88.55 mM; Need ultrasonic)

2

7

2

564.204 Da

564.204 Da

131.000 Ų

40

0

965

0

2