BI 1015550 (Nerandomilast) | PDE4B inhibitor | Probechem Biochemicals

Chemical Structure : BI 1015550

CAS No.: 1423719-30-5

加入收藏

BI 1015550 (Nerandomilast, VRN024219)

货号: PC-49676Not For Human Use, Lab Use Only.

BI 1015550 (Nerandomilast, VRN024219) is a potent, selective PDE4B inhibitor that preferentially inhibits hydrolysis of cAMP by PDE4B with IC50 of 10 nM, weakly inhibits PDE4A/4C/4D (IC50=248/8700/91 nM, respectively).

规格	价格	库存
5 mg	￥980	In stock
10 mg	￥1480	In stock
25 mg	￥2580	In stock
50 mg	￥4280	In stock
100 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

BI 1015550 (Nerandomilast, VRN024219) is a potent, selective PDE4B inhibitor that preferentially inhibits hydrolysis of cAMP by PDE4B with IC50 of 10 nM, weakly inhibits PDE4A/4C/4D (IC50=248/8700/91 nM, respectively).
BI 1015550 displays no significant activity agianst human PDE7A and human PDE3A, and PDE1C, PDE9A, human PDE2A and PDE5 at 10 uM.
BI 1015550 inhibited LPS-induced TNF- α release with an IC50 35 nM in human PBMCs, inhibited phytohemagglutinin P-induced IL-2 release with IC50 of 9 nM.
BI 1015550 completely inhibited LPS-stimulated TNF-α release with an IC50 in rat whole blood, inhibited TNF-α release up to 70–80% with an IC50 of 670 nM human whole blood.
BI 1015550 (0.01, 0.1, and 1 mg/kg, p.o.) inhibited LPS-stimulated TNF-α release in whole blood ex vivo in mice with ED50 of 0.04 mg/kg.
BI 1015550 (0.01, 0.1, and 1 mg/kg, p.o.) inhibited LPS-induced lung neutrophil influx in male Wistar rats with an ED50 of 0.1 mg/kg.
BI 1015550 inhibited α-SMA protein expression of TGF-β-stimulated IPF-LF with an IC50 of 210 nM, showed a synergistic effect in combination with Nintedanib on fibroblast proliferation.
BI 1015550 is a promising oral clinical candidate for the treatment of idiopathic pulmonary fibrosis (IPF) and other fibro-proliferative diseases.

物理化学性质&存储条件

分子量	448.97
分子式	C20H25ClN6O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	[1-({(5R)-2-[4-(5-chloropyrimidin-2-yl)piperidin-1-yl]-5-oxido-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl}amino)cyclobutyl]methanol

参考文献

1. Herrmann FE, et al. Front Pharmacol. 2022 Apr 20;13:838449.

BI 1015550 (Nerandomilast, VRN024219)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

BI 1015550 (Nerandomilast, VRN024219)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Get Quotation Now

* Indicates a Required FieldYour information is safe with us.