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Chemical Structure| 2242952-69-6 Chemical Structure| 2242952-69-6

Structure of BMS-986299
CAS No.: 2242952-69-6

Chemical Structure| 2242952-69-6

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BMS-986299 is an NLRP3 inflammasome activator with an EC50 of 1.28 μM. BMS-986299 activates the NLRP3 inflammasome and is used in research related to inflammatory diseases.

4.5 *For Research Use Only !

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Product Citations

Product Citations

Su, Yujing ; Wang, Hao ; Yang, Wenzhi ; Zhang, Shenhong ; Liu, Feifan ; Han, Kang , et al.

Abstract: Background: Spinal cord injury (SCI) leads to motor, sensory and autonomic dysfunction with no effective therapy till now. The malignant microenvironment and glial scars at the injury site impede neural circuit remodeling and functional recovery of SCI. Urolithin B (UB), an intestinal metabolite of ellagitannin, possesses anti-inflammatory, antioxidant, antitumor and neuropharmacological activities. Purpose: To investigate the effects and mechanism of UB in SCI recovery both in vitro and in vivo. Methods: At the cellular level, the study focused on the effects of UB on H2O2-induced PC12 cells damage and LPS-induced HMC3 cells polarization. At the in vivo level, the repair effect of UB gavage on SCI mice was performed by behavioral analysis, immunofluorescence, histopathology, and ELISA. Finally, network pharmacology, transcriptome sequencing, molecular docking, DARTS, and reverse validation were conducted to explore the molecular mechanism by which UB promotes SCI repair. Results: UB protected PC12 cells against H2O2-induced injury and decreased LPS-induced M1-type polarization of HMC3 cells. In addition, UB promoted nerve regeneration, regulated M1/M2 polarization of microglia, and reduced the formation of glial scars, thereby facilitating the motor function recovery of SCI mice. Further studies indicated that UB inhibited the NLRP3/Caspase-1/IL-1β pathway both in vivo and in vitro to reduce neuroinflammation. In contrast, BMS-986,299 (an agonist of NLRP3 inflammasome) attenuated the restorative effects of UB in SCI mice. Conclusion: UB inhibits the NLRP3/Caspase-1/IL-1β signaling pathway and M1 polarization of microglia to attenuate neuroinflammation and promote the functional recovery of SCI mice. Therefore, UB may be a potential therapeutic agent for the treatment of SCI.

Keywords: Spinal cord injury ; Urolithin B ; Neuroinflammation ; Glial scars ; NLRP3/Caspase-1/IL-1β signaling pathway

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Product Details of BMS-986299

CAS No. :2242952-69-6
Formula : C18H19N7O
M.W : 349.39
SMILES Code : CCN(C(C)=O)CC1=NC2=C(C(N)=NC3=C2C=CC(C4=CC=NN4)=C3)N1
MDL No. :MFCD34567729

Safety of BMS-986299

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
BV2 cells 5 μM 24 h To evaluate the effect of CPCGI on LPS-induced inflammatory response in BV2 cells, results showed that CPCGI significantly reduced IL-6 levels. CNS Neurosci Ther. 2025 Mar;31(3):e70322.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Traumatic brain injury (TBI) model Intraperitoneal injection 10 mg/kg/day Once daily until the end of the experiment To evaluate the effect of BMS-986299 on NLRP3 inflammasome activation in the TBI model, results showed that BMS-986299 reversed the neuroprotective effects of CPCGI. CNS Neurosci Ther. 2025 Mar;31(3):e70322.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.86mL

0.57mL

0.29mL

14.31mL

2.86mL

1.43mL

28.62mL

5.72mL

2.86mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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