BMX-001
Based on 1 Customer Validation
BMX-001 is a blood-brain barrier-penetrant, redox-active manganese porphyrin SOD mimetic with reactive oxygen species/reactive nitrogen species scavenging activity. BMX-001 inhibits NF-κB through S-glutathionylation, activates Nrf2/Keap1, and decreases TRPV1. BMX-001 enhances glucose-stimulated insulin secretion and inhibits islet apoptosis. BMX-001 radiosensitizes tumors, reduces cancer-associated fibroblasts, promotes dendritic cell maturation, modulates macrophage/MDSC/T cell responses, inhibits EMT/angiogenesis/hypoxia/inflammation, and induces apoptosis. BMX-001 protects glial cells while exerting pro-oxidant effects in cancer, and alleviates neuropathic pain. BMX-001 has neuroprotective effects in ischemic stroke. BMX-001 can be used for research on type 1 diabetes, ischemic stroke, pain, breast cancer, and glioblastoma.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 85%
- CAS No.: 1379783-91-1
- Formule: C64H76Cl5MnN8O4
- Masse moléculaire:1253.54
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
BMX-001 selectively kills LN-229 glioblastoma cells while sparing NHA normal human astrocytes, and reduces TNF-α and MnSOD in NHA cells after irradiation at 48 h[5].
BMX-001 (34 μM; 24 h) reduces mouse islet apoptosis; improves glucose-stimulated insulin secretion in mouse islets, with a stimulation index of 4.1[1].
BMX-001 (0.25-0.5 μM; 24 h) acts as a ROS scavenger in primary mouse SGCs, reducing PTX-induced total ROS; in MDA-MB-231 cells, it exerts a pro-oxidant effect, increasing PTX-induced ROS[4].
BMX-001 (0.25-0.5 μM; 24 h) preserves catalase and GPx activity in primary mouse SGCs while reducing PTX-induced SOD activity; in MDA-MB-231 cells, it impairs the antioxidant enzyme defense system under PTX-induced stress[4].
BMX-001 (50 µg/mL) does not alter t-PA-mediated clot lysis in an ex vivo rat arterial clot lysis assay[2].
BMX-001 co-incubation inhibits PTX-induced TNF-α and increases Nrf2 expression in primary mouse SGCs; it downregulates NF-κB expression in MDA-MB-231 cells without reducing PTX-induced TNF-α[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 human triple-negative breast cancer cells
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Concentration:0, 0.1, 0.25, 0.5, 1, 2 μM
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Incubation Time:24 h
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Result:For MDA-MB-231, 0.25 μM BMX-001 and 0.5 μM PTX were selected as safe concentrations for subsequent in vitro experiments based on cytotoxicity tests.
In Vivo
BMX-001 (34 µM; cultured in medium for 24 hours) improves engraftment of marginal human islet xenografts in immunodeficient B6-RAG-/- mice during human islet culture[1].
BMX-001 (10-34 µM; pancreatic distension/islet isolation and 24-hour culture) improves engraftment of marginal syngeneic islet transplants under the renal capsule of BALB/c mice during mouse islet isolation and culture[1].
BMX-001 (0.5 mg/kg; subcutaneous injection; on days 1, 3, 5, and 7, followed by twice weekly on days 9, 11, 15, and 18) in combination alleviates PTX-induced mechanical and thermal hyperalgesia and reduces neuroinflammation and oxidative stress markers in the DRG of CINP mice; the single agent does not alter mechanical or thermal sensitivity in healthy mice[4].
BMX-001 (30-225 µg/kg; subcutaneous injection after intracarotid administration; twice daily; 7 days) improves 7-day neurological deficits and reduces infarct volume in young male and female Wistar stroke rats[2].
BMX-001 (50-225 µg/kg; subcutaneous injection after intra-arterial administration; twice daily; 7 days) improves 28-day neurological functional recovery in young and aged SHR stroke rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (8-12 weeks old male donors; BALB/c recipients)[1]
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Dosage:10 µM and 34 µM
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Administration:supplemented during pancreas distension/islet isolation; 24-h culture
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Result:Improved marginal syngeneic islet engraftment under the kidney capsule in BALB/c mice, with 58% of recipients receiving 34 µM-supplemented islets becoming euglycemic.
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Animal Model:B6-RAG-/- (B6.129S7-Rag1tm1Mom/J)[1]
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Dosage:34 µM
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Administration:supplemented in culture medium; 24 h
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Result:Improved marginal human islet xenograft engraftment in immunocompromised B6-RAG-/- mice, with 92.3% of recipients receiving 34 µM-supplemented islets achieving euglycemia.
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Animal Model:Wistar (Hsd:WI, male, 250-275 g, 9 weeks old; female, 225-250 g, 9 weeks old)[2]
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Dosage:30 µg/kg; 225 µg/kg
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Administration:intra-carotid infusion over 5 min immediately after reperfusion; s.c. twice daily for 7 days
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Result:Improved 7-day neurological deficits and reduces infarct volume in young Wistar stroke rats.
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Animal Model:SHR (male, 225-250 g, 8 weeks old)
Fisher 344 (female, 220-250 g, 22 months old)[2] -
Dosage:50 µg/kg; 225 µg/kg
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Administration:intra-carotid infusion immediately after reperfusion; s.c. twice daily for 7 days
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Result:Improved 28-day neurological functional recovery.
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Animal Model:C57BL/6 (female, 56-62 days old, 18-21 g)[4]
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Dosage:0.5 mg/kg per dose (BMX-001); 8 mg/kg (PTX)
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Administration:BMX-001: s.c. on Days 1, 3, 5, and 7, then twice weekly on Days 9, 11, 15, and 18; PTX: i.p. on Days 1, 3, 5, and 7
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Result:Alleviated mechanical allodynia in CINP mice upon co‑administration of PTX and BMX‑001 in von Frey test.
Mitigated PTX‑evoked cold allodynia in acetone test and PTX‑induced thermal allodynia in hotplate test following combined PTX and BMX‑001 treatment.
Reduced PTX‑triggered upregulation of TRPV1, reversed elevated TNF‑α signal, and inhibited increased IBA‑1 expression in DRG tissues upon BMX‑001 intervention, with quantitative immunofluorescence intensity differences detected across experimental groups.
Prevented PTX‑mediated TNF‑α upregulation, boosted Nrf2 expression and suppressed PTX‑driven TRPV1 overexpression at DRG transcriptional level by BMX‑001 in qPCR assays, whereas PTX elevated TNF‑α and IL‑6 transcripts.
- Human pluripotent stem cell endothelial-cell differentiation
- Vascular/Branching Fractal Analysis
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- Human Islet Cell Culture
- Research Protocol for Inflammation-related Diseases
- Research Protocol for Metabolic Diseases
- Breast Cancer Modeling
- Research Protocol for Cancer Immunology
- Phagocytosis Functional Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Research Protocol for Endocrine Diseases
- Endothelial Tube Formation Assay
- Apoptosis Solutions
- Endothelial Cell Migration/Angiogenic Sprouting Assay
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1379783-91-1
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Appearance Solid
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Masse moléculaire 1253.54
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Formule C64H76Cl5MnN8O4
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Color Brown to black
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SMILES
CCCCOCC[N+]1=C(C=CC=C1)C2=C3C=CC4=C(C5=[N+](CCOCCCC)C=CC=C5)C6=[N]7[Mn+3]8([N-]34)[N-]9C(C(C%10=[N+](C=CC=C%10)CCOCCCC)=C%11C=CC2=[N]8%11)=CC=C9C(C%12=[N+](CCOCCCC)C=CC=C%12)=C7C=C6.[Cl-].[Cl-].[Cl-].[Cl-].[Cl-]
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 25 mg/mL (19.94 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (299 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Bruni A, et al. BMX-001, a novel redox-active metalloporphyrin, improves islet function and engraftment in a murine transplant model. American journal of transplantation : official journal of the American Society of Transplantation and the American Society of Transplant Surgeons. 2018 Aug;18(8):1879-1889. [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 (sealed storage, away from moisture). 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 | 0.7977 mL | 3.9887 mL | 7.9774 mL | 19.9435 mL |
| 5 mM | 0.1595 mL | 0.7977 mL | 1.5955 mL | 3.9887 mL | |
| 10 mM | 0.0798 mL | 0.3989 mL | 0.7977 mL | 1.9944 mL | |
| 15 mM | 0.0532 mL | 0.2659 mL | 0.5318 mL | 1.3296 mL |
BMX-001 Related Classifications
HY-125662A Related Classifications
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