BMS-986299
Based on 15 publication(s) in Google Scholar
BMS-986299 (compound 112) is a first-in-class NLRP3 inflammasome agonist with an EC50 of 1.28 μM. (patent WO2018152396A1).
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- 純度: 99.96%
- CAS 番号: 2242952-69-6
- 分子式: C18H19N7O
- 分子量:349.39
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 BMS-986299
More- Redox Biol. 2024 Jun 8:74:103225. [Abstract]
- Adv Healthc Mater. 2025 Nov 22:e03687. [Abstract]
- JCI Insight. 2026 Jan 27;11(5):e193017. [Abstract]
- CNS Neurosci Ther. 2025 Mar;31(3):e70322. [Abstract]
- Cell Mol Life Sci. 2024 Aug 19;81(1):359. [Abstract]
- Cancer Immunol Immunother. 2025 Jun 7;74(8):238. [Abstract]
- Int Immunopharmacol. 2026 Jun 25:186:117053. [Abstract]
- Int Immunopharmacol. 2026 Jan 1;168(Pt 2):115858. [Abstract]
- Mol Neurobiol. 2025 Jul 25. [Abstract]
- Inflammation. 2025 Jun;48(3):1159-1175. [Abstract]
- Front Pharmacol. 2022 Jul 5:13:906548. [Abstract]
- Neuropharmacology. 2023 Nov 15:239:109687. [Abstract]
- FASEB J. 2025 Nov 15;39(21):e71193. [Abstract]
- Histol Histopathol. 2025 Sep 22:18990. [Abstract]
- Physiol Rep. 2026 Apr;14(7):e70861. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
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WB
生物活性
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NLRP3 1.28 μM (EC50) |
BMS 986299 (1-1000 μM) shows low toxicity of cells PNRCMs[2].
BMS 986299 (1 μM, 1 h) upregulates the NLRP3 expression, stimulates the NLRP3 mediated cardiomyocyte pyroptosis in PNRCMs and therefore aggravates the DCM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2242952-69-6
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性状 Solid
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分子量 349.39
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分子式 C18H19N7O
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Color White to off-white
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SMILES
O=C(C)N(CC)CC1=NC2=C(N1)C3=C(C=C(C4=NNC=C4)C=C3)N=C2N
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (15)
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Journal Impact Factor
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Most Recent
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Redox Biol
FAM3A plays a key role in protecting against tubular cell pyroptosis and acute kidney injury. [Abstract]2024 Jun 8:74:103225. PMID: 38875957 -
Adv Healthc Mater
Regulation of Inflammatory and Metabolic Microenvironment With a D-Mannose Functionalized Hydrogel for Improved Osteochondral Regeneration. [Abstract]2025 Nov 22:e03687. PMID: 41273165 -
JCI Insight
USP16 drives psoriasis progression by deubiquitinating and stabilizing NLRP3 in keratinocytes. [Abstract]2026 Jan 27;11(5):e193017. PMID: 41591834 -
CNS Neurosci Ther
CPCGI Alleviates Neural Damage by Modulating Microglial Pyroptosis After Traumatic Brain Injury. [Abstract]2025 Mar;31(3):e70322. PMID: 40059065 -
Cell Mol Life Sci
SGK3 deficiency in macrophages suppresses angiotensin II-induced cardiac remodeling via regulating Ndufa13-mediated mitochondrial oxidative stress. [Abstract]2024 Aug 19;81(1):359. PMID: 39158709 -
Cancer Immunol Immunother
NLRP3 activation promotes cGAS/STING signaling and antitumor immunity by colorectal cancer cells. [Abstract]2025 Jun 7;74(8):238. PMID: 40481953 -
Int Immunopharmacol
Repurposing AZD-7762 as a novel direct NLRP3 inhibitor for the treatment of inflammatory diseases. [Abstract]2026 Jun 25:186:117053. PMID: 42348984 -
Int Immunopharmacol
STING knockdown blocks disease progression and inflammation in mice with alcoholic liver disease by relieving pyroptosis via suppressing NLRP3. [Abstract]2026 Jan 1;168(Pt 2):115858. PMID: 41265219 -
Mol Neurobiol
Syringaldehyde Ameliorates Cognitive Dysfunction in APP/PS1 Mice by Stabilizing the NLRP3 Pathway. [Abstract]2025 Jul 25. PMID: 40711709 -
Inflammation
Dichloroacetate Prevents Sepsis Associated Encephalopathy by Inhibiting Microglia Pyroptosis through PDK4/NLRP3. [Abstract]2025 Jun;48(3):1159-1175. PMID: 39177920 -
Front Pharmacol
Cyclovirobuxine D Ameliorates Experimental Diabetic Cardiomyopathy by Inhibiting Cardiomyocyte Pyroptosis via NLRP3 in vivo and in vitro. [Abstract]2022 Jul 5:13:906548. PMID: 35865939
BMS-986299 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2022 Jul 5:13:906548. [Abstract]
Cytotoxicity of BMS-986299(1, 10, 100, 1000 μM ) as detected by MTT assay.
BMS-986299 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2022 Jul 5:13:906548. [Abstract]
LDH content in cell culture supernatant was detected after pretreatment with BMS-986299 (1 μM).
BMS-986299 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2022 Jul 5:13:906548. [Abstract]
The effect of BMS-986299 (1 μM) on cardiomyocyte pyroptosis was observed by PI staining.
BMS-986299 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2022 Jul 5:13:906548. [Abstract]
Western blotting was used to detected proteins expression in pyroptosis pathway with BMS-986299 (1 μM) pretreatment.
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Neuropharmacology
HET0016 inhibits neuronal pyroptosis in the immature brain post-TBI via the p38 MAPK signaling pathway. [Abstract]2023 Nov 15:239:109687. PMID: 37579871 -
FASEB J
Senkyunolide I Alleviated Renal Fibrosis in UUO Mice by Regulating the Nrf2/xCT/GPX4 and NLRP3/Caspase-1/GSDMD Pathways to Inhibit Ferroptosis and Pyroptosis. [Abstract]2025 Nov 15;39(21):e71193. PMID: 41148161 -
Histol Histopathol
Penning decoction ameliorated pyroptosis in mice with lipopolysaccharide-induced endometritis through inhibition of the TLR4/NF-κB/NLRP3 pathway. [Abstract]2025 Sep 22:18990. PMID: 40977347 -
Physiol Rep
Mechanism of paraventricular nucleus H2S on PERK/TXNIP/NLRP3 pathway in male spontaneously hypertensive rats. [Abstract]2026 Apr;14(7):e70861. PMID: 41964264
溶剤 & 溶解度
DMSO : 33.33 mg/mL (95.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (251 KB)
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- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Gary Glick, et al. Substituted imidazo-quinolines as nlrp3 modulators. WO2018152396A1.
[2]. Gao G, et al., Cyclovirobuxine D Ameliorates Experimental Diabetic Cardiomyopathy by Inhibiting Cardiomyocyte Pyroptosis via NLRP3 in vivo and in vitro. Front Pharmacol. 2022 Jul 5;13:906548. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8621 mL | 14.3107 mL | 28.6213 mL | 71.5533 mL |
| 5 mM | 0.5724 mL | 2.8621 mL | 5.7243 mL | 14.3107 mL | |
| 10 mM | 0.2862 mL | 1.4311 mL | 2.8621 mL | 7.1553 mL | |
| 15 mM | 0.1908 mL | 0.9540 mL | 1.9081 mL | 4.7702 mL | |
| 20 mM | 0.1431 mL | 0.7155 mL | 1.4311 mL | 3.5777 mL | |
| 25 mM | 0.1145 mL | 0.5724 mL | 1.1449 mL | 2.8621 mL | |
| 30 mM | 0.0954 mL | 0.4770 mL | 0.9540 mL | 2.3851 mL | |
| 40 mM | 0.0716 mL | 0.3578 mL | 0.7155 mL | 1.7888 mL | |
| 50 mM | 0.0572 mL | 0.2862 mL | 0.5724 mL | 1.4311 mL | |
| 60 mM | 0.0477 mL | 0.2385 mL | 0.4770 mL | 1.1926 mL | |
| 80 mM | 0.0358 mL | 0.1789 mL | 0.3578 mL | 0.8944 mL |
BMS-986299 関連分類
HY-139396 関連分類
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