| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
M1001 targets the hypoxia-inducible factor-2α (HIF-2α). It binds directly to the HIF-2α PAS-B domain with a Kd of 667 nM. This binding enhances the stability of the HIF-2α-ARNT complex. By stabilizing the complex, M1001 promotes the gene expression of HIF-2α targets such as VEGF-A and NDRG1. It acts as a modulator of the HIF-2α pathway.
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| ln Vitro |
In 786-O cells, M1001 (10 μM) treatment resulted in enhanced expression of HIF-2 target genes [1]. M1001 (10 μM) demonstrates mild pulsatile effects upon binding to HIF-2α [1]. M1001 (1–10 μM)
In vitro, M1001 promotes the gene expression of HIF-2α targets VEGF-A and NDRG1 in 786-O cells at a concentration of 10 µM. It binds to the HIF-2α PAS-B domain. It is used to study the role of HIF-2α in cellular responses to hypoxia. It is a valuable tool for exploring the HIF pathway in both cellular and animal models. Its activity has applications in oncology and metabolic disease research. |
| ln Vivo |
In vivo, M1001 is used to study the HIF-2α signaling pathway in animal models. It can be used to investigate the role of HIF-2α in various diseases, including chronic kidney disease. By activating HIF-2α, it can help elucidate the effects of this pathway on erythropoiesis, angiogenesis, and metabolism. The compound's ability to modulate HIF-2α makes it a useful tool for studying hypoxia-related pathologies.
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| Enzyme Assay |
The in vitro binding assay for M1001 involves measuring its affinity for the HIF-2α PAS-B domain using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). Varying concentrations of M1001 (1 nM-100 µM) are tested. The Kd is determined from the binding curves. Cell-based assays measure the induction of HIF-2α target genes (e.g., VEGF-A, NDRG1) by qPCR in cells treated with M1001 (1-100 µM) for 6-24 hours.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: 786-O Cell Tested Concentrations: 10 μM Incubation Duration: Experimental Results: Moderate increase in expression of HIF-2 target genes in 786-O cells) Reduce VHL and HIF-2α combination [1]. . Western Blot Analysis[1] Cell Types: HEK293T Cell Tested Concentrations: 1 and 10 µM Incubation Duration: Experimental Results: diminished physical association between HIF-2α and VHL. In vitro cellular assays for M1001 use cell lines such as 786-O renal carcinoma cells. Cells are treated with M1001 at concentrations of 1-100 µM for 6-24 hours. The expression of HIF-2α target genes is measured by qPCR or Western blot. Cell viability is assessed using MTT assays. The compound's effect on cell proliferation and migration can be evaluated. These assays help characterize the compound's activity as a HIF-2α agonist. |
| Animal Protocol |
In vivo animal studies for M1001 involve mouse models of disease. The compound is administered via oral gavage or intraperitoneal injection at doses of 1-50 mg/kg. Target gene expression (e.g., VEGF-A, EPO) is measured in tissues. The compound's effects on physiological parameters, such as hematocrit, are assessed. These studies help validate the role of HIF-2α in various disease models and assess the compound's in vivo efficacy.
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| ADME/Pharmacokinetics |
M1001 has a molecular weight of 327.4 and a molecular formula of C17H17N3O2S. It is a weak HIF-2α agonist with a Kd of 667 nM. It binds to the HIF-2α PAS-B domain. It is a research tool for studying hypoxia signaling. The compound is not for human therapeutic use.
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| References |
| Molecular Formula |
C17H17N3O2S
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|---|---|
| Molecular Weight |
327.400782346725
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| Exact Mass |
327.104
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| CAS # |
874590-32-6
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| PubChem CID |
4905675
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| Appearance |
Light green to green solid powder
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| LogP |
2.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
563
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=S1(C2C(=CC=CC=2)C(NC2C(N3CCCC3)=CC=CC=2)=N1)=O
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| InChi Key |
LONXCUOJVJLTIP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17N3O2S/c21-23(22)16-10-4-1-7-13(16)17(19-23)18-14-8-2-3-9-15(14)20-11-5-6-12-20/h1-4,7-10H,5-6,11-12H2,(H,18,19)
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| Chemical Name |
1,1-dioxo-N-(2-pyrrolidin-1-ylphenyl)-1,2-benzothiazol-3-amine
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| Synonyms |
M-1001; M 1001; M1001
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~763.59 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.33 mg/mL (7.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 23.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0544 mL | 15.2718 mL | 30.5437 mL | |
| 5 mM | 0.6109 mL | 3.0544 mL | 6.1087 mL | |
| 10 mM | 0.3054 mL | 1.5272 mL | 3.0544 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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