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Chemical Structure| 433695-36-4 Chemical Structure| 433695-36-4

Structure of BRL-50481
CAS No.: 433695-36-4

Chemical Structure| 433695-36-4

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BRL-50481 is an inhibitor of PDE7 with IC50 of 0.15 μM and can also inihibt PDE7A, PDE7B, PDE4 and PDE3. BRL-50481 has been shown to increase mineralisation activity in osteoblasts thus has the potential treatment of osteoporosis.

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Product Details of BRL-50481

CAS No. :433695-36-4
Formula : C9H12N2O4S
M.W : 244.27
SMILES Code : O=S(C1=CC([N+]([O-])=O)=CC=C1C)(N(C)C)=O
MDL No. :MFCD03039912
InChI Key :IFIUFCJFLGCQPH-UHFFFAOYSA-N
Pubchem ID :2921148

Safety of BRL-50481

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
rat aortic smooth muscle cells (RASMCs) 50 μM 3 min To evaluate the role of PDE7 in regulating cAMP signals, results showed BRL had minor effects on the kinetics of Iso-induced FRET signal (time to peak increased by 17%) PLoS One. 2012;7(10):e47826
OPCs isolated from adult human brain biopsies 1 μM 5 days To investigate the effects of PDE7 inhibitors on human OPC differentiation, results showed that VP1.15 and TC3.6 significantly promoted OPC differentiation into oligodendrocytes. Cell Mol Life Sci. 2013 Sep;70(18):3449-62
EHEB cells 30 µM 48 h Assess the effect of BRL-50481 on proliferation of EHEB cells; results show it inhibits proliferation by 19±1%. Proc Natl Acad Sci U S A. 2008 Dec 9;105(49):19532-7
CLL cells 30 µM 48 h Evaluate the effect of PDE7 inhibitors on apoptosis of CLL cells; results show BRL-50481 significantly induces apoptosis in CLL cells. Proc Natl Acad Sci U S A. 2008 Dec 9;105(49):19532-7

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Male BALB/c mice ConA-induced autoimmune hepatitis model Intraperitoneal injection 50 mg/kg Single dose, hepatitis induced 30 minutes later To evaluate the anti-inflammatory and hepatoprotective effects of BRL-50481 in the ConA-induced hepatitis model. Results showed that BRL-50481 significantly reduced serum TNF-α and IL-17 levels and alleviated liver injury. J Pharmacol Exp Ther. 2022 May;381(2):151-163
SJL mice Experimental autoimmune encephalomyelitis (EAE) Intraperitoneal injection 10 μg/g body weight Daily administration, starting from the day of MBP inoculation (D0) Evaluate the therapeutic effect of BRL50481 on EAE, results showed BRL50481 had no effect on the disease course Br J Pharmacol. 2013 Oct;170(3):602-13
C57BL/6J mice Partial sciatic nerve ligation (PSNL) and complete Freund’s adjuvant (CFA) induced chronic pain and depression models Oral 10 mg/kg Once daily for 14-33 days BRL50481 significantly alleviated PSNL- or CFA-induced mechanical hypersensitivity and depression-like behavior and reversed the downregulation of cAMP-PKA-CREB-BDNF signaling and increased neuroinflammation in the hippocampus. Int J Neuropsychopharmacol. 2024 Oct 1;27(10):pyae040
BALB/c mice OVA-induced asthmatic lung inflammation model Intraperitoneal injection 2 mg/kg Administered 1 hour before each challenge, total of 6 times BRL significantly reduced AHR, infiltration of inflammatory cells, Th2-related cytokines, antigen-specific immunoglobulins, and mucin levels, ameliorating OVA-induced allergic asthmatic responses. Arch Pharm Res. 2022 Jan;45(1):51-62

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.09mL

0.82mL

0.41mL

20.47mL

4.09mL

2.05mL

40.94mL

8.19mL

4.09mL

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