| Identification | Back Directory | [Name]
LDN-27219 | [CAS]
312946-37-5 | [Synonyms]
184663
CS-1194
LDN-27219
LDN-27219
(LDN 27219
LDN-27219 >=98% (HPLC)
2-({4-oxo-3,5-diphenyl-3H,4H-thieno[2,3-d]pyrimid in-2-yl}sulfanyl)acetohydrazide
2-((4-oxo-3,5-diphenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio)acetohydrazide
2-[(3,4-Dihydro-4-oxo-3,5-diphenylthieno[2,3-d]pyrimidin-2-yl)thio]-acetic acid hydrazide
Acetic acid, 2-[(3,4-dihydro-4-oxo-3,5-diphenylthieno[2,3-d]pyrimidin-2-yl)thio]-, hydrazide | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C20H16N4O2S2 | [MOL File]
312946-37-5.mol | [Molecular Weight]
408.5 |
| Chemical Properties | Back Directory | [density ]
1.45±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMSO: soluble15mg/mL, clear | [form ]
powder | [pka]
11.87±0.37(Predicted) | [color ]
white to beige | [InChI]
1S/C20H16N4O2S2/c21-23-16(25)12-28-20-22-18-17(15(11-27-18)13-7-3-1-4-8-13)19(26)24(20)14-9-5-2-6-10-14/h1-11H,12,21H2,(H,23,25) | [InChIKey]
WLBUICQBNZXIDJ-UHFFFAOYSA-N | [SMILES]
[s]1c2nc([n]([c](c2c(c1)c4ccccc4)=O)c3ccccc3)SCC(=O)NN |
| Hazard Information | Back Directory | [Uses]
LDN 27219 is a transglutaminase inhibitor. | [Biological Activity]
LDN-27219 is a revesible inhibitor of transglutaminase 2 (TG2) th at binds to the GTP binidng site of the enzyme and inhbits activity with and IC50 of 600 nM.''LDN-27219 is a thieno[2,3-d]pyrimidine-4-one-acylhydrazide derivative. Closed conformation of TG2 induced by LDN-27219 can be a potential therapeutic strategy for age-related vascular dysfunction and lowering blood pressure. | [in vivo]
LDN-27219 (0.1-2 mg/kg; i.v. once) affects vivo arterial pressure and shows larger effects on older rats[2]. | Animal Model: | 12 to 14-week-old male Wistar rats[2] | | Dosage: | 0.1, 1 and 2 mg/kg | | Administration: | Intravenous injection; 0.1, 1 and 2 mg/kg once | | Result: | Dose-dependently decreased mean arterial pressure of mice. |
| Animal Model: | 12 to 14- and 35 to 40-week-old male Wistar rats | | Dosage: | 0.1, 1 and 2 mg/kg | | Administration: | Intravenous injection; 0.1, 1 and 2 mg/kg once | | Result: | Decreased mean arterial pressure in old group more significant than young group. |
| [storage]
Store at +4°C |
|
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