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
- Product 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 No.
- 568580-02-9
- Chemical 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
- 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
- CBNumber
- CB15490212
- Molecular Formula
- C46H69N7O15
- Formula Weight
- 960.09
- MOL File
- 568580-02-9.mol
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 Property
- 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.
N-Bromosuccinimide Price
- Product number
- 29735
- Product name
- YM-254890
- Packaging
- 1mg
- Price
- $335
- Updated
- 2024/03/01
- Product number
- AG-CN2-0509-M001
- Product name
- YM-254890
- Purity
- ≥95%(HPLC)
- Packaging
- 1mg
- Price
- $370
- Updated
- 2021/12/16
- Product number
- CS-0087171
- Product name
- YM-254890
- Purity
- ≥99.0%
- Packaging
- 250ug
- Price
- $250
- Updated
- 2021/12/16
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 Chemical Properties,Usage,Production
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.
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]
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 Preparation Products And Raw materials
Raw materials
Preparation Products
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 Suppliers
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