| Identification | Back Directory | [Name]
L-Threonine, N-acetyl-L-threonyl-(αR)-α-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-2-(acetylamino)-3-hydroxy-4-methyl-1-oxopentyl]oxy]-L-leucyl-N,O-dimethyl-, (7→1)-lactone | [CAS]
568580-02-9 | [Synonyms]
L-Threonine, N-acetyl-L-threonyl-(αR)-α-hydroxybenzenepropanoyl-2,3-didehydro-N-methylalanyl-L-alanyl-N-methyl-L-alanyl-(3R)-3-[[(2S,3R)-2-(acetylamino)-3-hydroxy-4-methyl-1-oxopentyl]oxy]-L-leucyl-N,O-dimethyl-, (7→1)-lactone | [Molecular Formula]
C46H69N7O15 | [MDL Number]
MFCD09832722 | [MOL File]
568580-02-9.mol | [Molecular Weight]
960.08 |
| Chemical Properties | Back Directory | [Boiling point ]
1232.4±65.0 °C(Predicted) | [density ]
1.26±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (up to 10 mg/ml) | [form ]
lyophilized solid | [pka]
12.52±0.70(Predicted) | [color ]
White or off-white | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| Hazard Information | Back Directory | [Description]
YM-254890 (568580-02-9) is a novel Gαq/11 inhibitor.1 U46619-induced platelet aggregation is inhibited but phorbol ester- or ionophore-induced aggregation is not2 (IC50 = 0.1-0.2 μM)1. It blocks Pasteurella multocida toxin-mediated activation of Gαq.3 A highly useful new tool for studying Gαq/11-coupled receptor signaling and resulting cellular events.4 | [Uses]
YM-254890 is a selective inhibitor of Gαq. | [IC 50]
P2Y1 Receptor | [storage]
Store at -20°C | [References]
1) Takasaki (2004), A novel Galphaq/11-selective inhibitor; J. Biol. Chem., 279 47438
2) Uemura et al. (2006), Biological properties of a specific Galpha q/11 inhibitor, YM-254890, on platelet functions and thrombus formation under high-shear stress; Br. J. Pharmacol., 148 61
3) Orth et al. (2005), Pasteurella multocida toxin-induced activation of RhoA is mediated via two families of G{alpha} proteins, G{alpha}g and G{alpha}12/13; J. Biol. Chem., 280 36701
4) Mizuno and Itoh (2009), Functions and regulatory mechanisms of Gq-signaling pathways; Neurosignals, 17 42
5) Kankanamge et al. (2018) Melanopsin (Opn4) utilizes Gαi Gβγ as major signal transducers; J. Cell Sci., 131 Jcs212910 [Focus Citation]
6) Pera et al. (2018) Biased signaling of the proton-sensing receptor OGR1 by benzodiazepines; FASEB J., 32 862[Focus Citation]
7) Ratnayake et al. (2018) Blue light excited retina intercepts cellular signaling; Sci. Rep. 8 10207[Focus Citation]
8) Zimering and Nadkami (2019)?Schizophrenia Autoantibodies Promote? “Biased agonism” at the 5-Hydroxytryptamine? 2A Receptor: Neurotoxicity is Positively Modulated by Metabotropic? Glutamate 2/3 Receptor Agonism; Endocrinol. Diabetes Metab. J., 3 1 [Focus Citation] |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
R&D Systems, Inc
|
| Tel: |
18003437475 18003437475 |
| Website: |
www.rndsystems.com |
| Company Name: |
Enzo Biochem Inc
|
| Tel: |
Enzo Biochem Inc. 13797054060 |
| Website: |
www.enzo.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|