| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
| ln Vitro |
BRD-6929 uses recombinant human HDAC enzymes and HDAC class-specific substrates to demonstrate the in vitro IC50 for HDAC1-9. To regulate HDAC1-3 inhibition, BRD-6929 was incubated with substrate (HDAC1-3) for 180 minutes. For HDAC1, HDAC2, HDAC3, and HDAC4-9, BRD-6929 exhibits IC50 values of 0.001 µM, 0.008 µM, 0.458 µM, and >30, correspondingly. µM[1]. HDACs 1, 2, and 3 treated with BRD-6929 (10 µM) showed in vitro binding affinity (Ki) and kinetics (half-life "T1/2" in minutes); Ki values for HDAC 1, 2, and 3 were <0.2 nM, 1.5 nM, and 270 nM, respectively. For HDAC 1, 2, and 3, the corresponding T1/2 values are >2400 minutes, >4800 minutes, and 1200 minutes [1]. Primary cultures of certain brain regions did not show an increase or decrease in the total number of cells in response to BRD-6929 (1 and 10 uM). Furthermore, in primary cultures of the striatum, a brain region-specific culture, BRD-6929 (10 uM) increases H4K12 acetylation [1]. In primary neuronal cell cultures, BRD-6929 (1-10 uM; 6 hours) significantly increases H2B acetylation. With an EC50 of 7.2 µM, BRD-6929 (1–20 uM; 24 hours) causes dose-dependent H4K12ac acetylation in cultured neurons [1]. The PKC agonist genidimarin is more effective against latent HIV-1 when combined with BRD-6929 [3].
|
|---|---|
| ln Vivo |
BRD-6929 (ip; 45 mg/kg; single dose) had Cmax, T1/2, and AUC values in plasma of 17.7 μM, 7.2 hours, and 25.6 μM/L*hr, in that order. According to reference [1], the brain exhibits Cmax, T1/2, and AUC values of 0.83 μM, 6.4 hours, and 3.9 μM/L*hr, respectively. In the mouse brain, BRD-6929 (ip; 45 mg/kg; 10 days) functions as a deacetylase inhibitor. In comparison to the vehicle, it markedly raised acetylation in every brain region by 1.5–2.0 times. In the brain, ventral striatum, and hippocampus of adult male C57BL/6J mice, BRD-6929 dramatically elevated the acetylation of histones H2B (tetraacetylation), H3K9, and H4K12 on day 10 of therapy, according to Western blotting [1].
|
| References | |
| Additional Infomation |
4-acetamido-N-(2-amino-5-thiophen-2-ylphenyl)benzamide is a member of benzamides.
|
| Molecular Formula |
C19H17N3O2S
|
|---|---|
| Molecular Weight |
351.422182798386
|
| Exact Mass |
351.104
|
| CAS # |
849234-64-6
|
| PubChem CID |
6918878
|
| Appearance |
Off-white to gray solid powder
|
| LogP |
4.935
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
25
|
| Complexity |
479
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ABZSPJVXTTUFAA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H17N3O2S/c1-12(23)21-15-7-4-13(5-8-15)19(24)22-17-11-14(6-9-16(17)20)18-3-2-10-25-18/h2-11H,20H2,1H3,(H,21,23)(H,22,24)
|
| Chemical Name |
4-acetamido-N-(2-amino-5-thiophen-2-ylphenyl)benzamide
|
| 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 : ~5 mg/mL (~14.23 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.92 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 20.8 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 | 2.8456 mL | 14.2280 mL | 28.4560 mL | |
| 5 mM | 0.5691 mL | 2.8456 mL | 5.6912 mL | |
| 10 mM | 0.2846 mL | 1.4228 mL | 2.8456 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
