| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
| Targets |
HIV-1
|
|---|---|
| ln Vitro |
Cultured PBMCs are susceptible to dose-dependent apoptosis when exposed to Ro 24-7429 (0.1–5 μM) for three days.
Moreover, Ro 24-7429 (1–25 μM) suppresses antigen-induced lymphocyte proliferation and causes apoptosis[1].
In a dose-dependent manner, Ro24-7429 (50-200 μM; 24-72 hours) strongly inhibits the proliferation of A549 and HLF cells. TNF-α-induced up-regulation of RUNX1 mRNA is significantly reduced by 50% after 48 hours with Ro24-7429 treatment at 75 μM[2]. |
| ln Vivo |
In the Bleomycin-induced pulmonary fibrosis (PF) mouse model, treatment with Ro24-7429 (17.5-70 mg/kg; i.p.; daily; for 14 or 21 days) significantly reduces lung inflammation and fibrosis. In injured mouse lungs, Ro24-7429 reduces the expression of fibrosis markers[2].
|
| Animal Protocol |
Animal Model: Bleomycin-induced male and female C57BL/6J mice (aged 6–8 weeks)[2]
Dosage: 17.5 mg/kg, 35 mg/kg, and 70 mg/kg Administration: i.p.; daily; for 14 or 21 days Result: reduced inflammation and lung fibrosis in the PF mouse model induced by bleomycin. |
| References |
|
| Additional Infomation |
7-chloro-N-methyl-5-(1H-pyrrol-2-yl)-3H-1,4-benzodiazepin-2-amine is a benzodiazepine.
Ro 24-7429 is under investigation in clinical trial NCT00002314 (A Study of Ro 24-7429 in Patients With Hiv-related Kaposi's Sarcoma). |
| Molecular Formula |
C14H13CLN4
|
|---|---|
| Molecular Weight |
272.74
|
| Exact Mass |
272.083
|
| Elemental Analysis |
C, 61.65; H, 4.80; Cl, 13.00; N, 20.54
|
| CAS # |
139339-45-0
|
| Related CAS # |
139339-45-0; 2328140-37-8; 30195-30-3;
|
| PubChem CID |
135422895
|
| Appearance |
White to yellow solid powder
|
| Density |
1.36g/cm3
|
| Boiling Point |
514.6°C(760mmHg),计算值
|
| Flash Point |
265°C
|
| LogP |
2.03
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
19
|
| Complexity |
393
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CNC1CN=C(C2=CC=CN2)C2C=C(C=CC=2N=1)Cl
|
| InChi Key |
LEAKQIXYSHIHCW-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H13ClN4/c1-16-13-8-18-14(12-3-2-6-17-12)10-7-9(15)4-5-11(10)19-13/h2-7,17H,8H2,1H3,(H,16,19)
|
| Chemical Name |
3H-1,4-Benzodiazepin-2-amine, 7-chloro-N-methyl-5-(1H-pyrrol-2-yl)-
|
| Synonyms |
Ro247429; Ro247429; Ro-247429; Ro 247429;Ro 24-7429; Ro-24-7429;
|
| 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 : ~62.5 mg/mL (~229.16 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.63 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saliney: ≥ 2.08 mg/mL (7.63 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6665 mL | 18.3325 mL | 36.6650 mL | |
| 5 mM | 0.7333 mL | 3.6665 mL | 7.3330 mL | |
| 10 mM | 0.3666 mL | 1.8332 mL | 3.6665 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00002314 | COMPLETED | Drug: Ro 24-7429 | HIV Infections Sarcoma, Kaposi |
Hoffmann-La Roche | Phase 2 | |
| NCT00000760 | COMPLETED | Drug: Ro 24-7429 Drug: Zidovudine Drug: Didanosine |
HIV Infections | National Institute of Allergy and Infectious Diseases (NIAID) | Phase 1 |
|
|
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
