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Mirabegron free base

Mirabegron is a selective β3-adrenoceptor agonist.

For research use only. Not for human or veterinary use.

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Mirabegron structure

CAS No.: 223673-61-8

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
100 mg USD 480.00 BP-02316-100mg In stock Get quote
250 mg USD 950.00 BP-02316-250mg In stock Get quote
500 mg USD 1,420.00 BP-02316-500mg In stock Get quote
1 g USD 2,460.00 BP-02316-1g In stock Get quote
2 g USD 3,930.00 BP-02316-2g In stock Get quote
3 g USD 4,710.00 BP-02316-3g In stock Get quote
5 g USD 6,290.00 BP-02316-5g In stock Get quote

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Description

Mirabegron is a selective β3-adrenoceptor agonist with EC50 of 22.4 nM.

Biological activity

In Vitro Mirabegron (YM178) increases cyclic AMP accumulation in Chinese hamster ovary (CHO) cells expressing human β3-adrenoceptor (AR). EC50 value is 22.4 nM. EC50 values of Mirabegron for human β1- and β2-ARs are 10,000 nM or more, respectively. EC50 of Mirabegron in rat bladder strips precontracted with 10-6 M Carbachol (CCh) is 5.1 μM, whereas that in human bladder strips precontracted with 10-7 M CCh is 0.78 μM. Mirabegron concentration-dependently increases the accumulation of cAMP in CHO cells expressing human β3-ARs, with an EC50 value and I.A. of 22.4 nM and 0.8, respectively. Mirabegron has little agonistic effect on β1- and β2-ARs. Compared by EC50 value, Mirabegron is approximately one third as potent as isoproterenol. The maximal relaxant effects of Mirabegron are 94±1%, that of CCh, indicating that Mirabegron acts a full agonist in the rat bladder. The maximal relaxant effects of Mirabegron is 89.4±2.3%. In Vivo Mirabegron (YM178) produces a dose-dependent decrease in the frequency of rhythmic bladder contraction in anesthetized rats. In contrast, Mirabegron does not decrease the amplitude of rhythmic bladder contraction at up to 3 mg/kg i.v.. On the contrary, Oxybutynin significantly increases the frequency of rhythmic bladder contraction and decreased its amplitude at doses of 0.272 mg/kg i.v. or more.

Identifiers

SMILES
NC1=NC(CC(=O)NC2=CC=C(CCNC[C@H](O)C3=CC=CC=C3)C=C2)=CS1
InChIKey
PBAPPPCECJKMCM-IBGZPJMESA-N

Specifications

MW (average)
396.5060
Formula
C21H24N4O2S
CAS No.
223673-61-8
Physical state
Solid
Color
white to light yellow
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder 4℃ 2 years; In solvent -20℃ 1 month;

References

[1]. Takasu T, et al. Effect of (R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl} acetanilide (YM178), a novel selective beta3-adrenoceptor agonist, on bladder function. J Pharmacol Exp Ther. 2007 May;321(2):642-7.

Same research area

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