| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
CID-1067700 (CID1067700) is a novel and potent pan GTPase inhibitor that can competitively inhibit Ras-related in brain 7 (Rab7) with a Ki of 13 nM.
| Targets |
|
|
|---|---|---|
| ln Vitro |
With a Ki of 13 nM, CID-1067700 (ML282), a pan-GTPase inhibitor, inhibits Rab7 in a competitive manner. Rab7 nucleotide binding is inhibited by CID-1067700, with Kd values of 40 nM and 100 nM for BODIPY-GDP and BODIPY-GTP, respectively. CID-1067700 substantially inhibits BODIPY-linked nucleotide binding as concentration rises. BODIPY-GTP has an EC50 value of 11.22 nM, while BODIPY-GDP has an EC50 value of 20.96 ± 1.34 nM. The computed values of Ki are 19.70 and 12.89 nM, respectively. M. Under equilibrium binding settings, CID-1067700 (10 μM) has no effect on the release rate of wild-type Rab7-bound BODIPY-linked nucleotides [1]. In B cells, CID-1067700 (0–40 μM) suppresses AID induction, NF-κB activation, and Rab7 activity. Additionally, CID-1067700 targets Rab7 to bind it with high affinity (EC50=10–20 nM) and prevent class switch DNA recombination (CSR) in B cells [2].
|
|
| ln Vivo |
By inhibiting Rab7, CID-1067700 (ML282; 16 mg/kg, i.p.) stops the progression of lupus-prone mice's disease and lowers IgG-IC deposition in MRL/Faslpr/lpr mice. Additionally focusing on B cells, CID-1067700 directly impairs the body's CSR mechanism [2].
|
|
| Cell Assay |
|
|
| References |
|
|
| Additional Infomation |
2-[[benzamido(sulfanylidene)methyl]amino]-5,5-dimethyl-4,7-dihydrothieno[2,3-c]pyran-3-carboxylic acid is a thienopyran.
|
| Molecular Formula |
C18H18N2O4S2
|
|---|---|
| Molecular Weight |
390.47652
|
| Exact Mass |
390.07
|
| CAS # |
314042-01-8
|
| PubChem CID |
1067700
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Index of Refraction |
1.681
|
| LogP |
4.76
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
26
|
| Complexity |
578
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ATSWBWHRHAQVFM-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H18N2O4S2/c1-18(2)8-11-12(9-24-18)26-15(13(11)16(22)23)20-17(25)19-14(21)10-6-4-3-5-7-10/h3-7H,8-9H2,1-2H3,(H,22,23)(H2,19,20,21,25)
|
| Chemical Name |
2-(benzoylcarbamothioylamino)-5,5-dimethyl-4,7-dihydrothieno[2,3-c]pyran-3-carboxylic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~32.01 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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 | 2.5610 mL | 12.8048 mL | 25.6095 mL | |
| 5 mM | 0.5122 mL | 2.5610 mL | 5.1219 mL | |
| 10 mM | 0.2561 mL | 1.2805 mL | 2.5610 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
