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MedKoo Cat#: 526182 | Name: Ro 24-7429
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Ro 24-7429 is a Tat antagonist. Ro 24-7429 blocks the action of the HIV tat protein and is an analog of Ro 5-3335.

Chemical Structure

Ro 24-7429
Ro 24-7429
CAS#139339-45-0

Theoretical Analysis

MedKoo Cat#: 526182

Name: Ro 24-7429

CAS#: 139339-45-0

Chemical Formula: C14H13ClN4

Exact Mass: 272.0829

Molecular Weight: 272.74

Elemental Analysis: C, 61.65; H, 4.80; Cl, 13.00; N, 20.54

Price and Availability

Size Price Availability Quantity
5mg USD 190.00 Ready to ship
10mg USD 350.00 Ready to ship
25mg USD 650.00 Ready to ship
50mg USD 1,150.00 Ready to ship
100mg USD 1,850.00 Ready to ship
200mg USD 2,950.00 Ready to ship
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Related CAS #
139339-45-0 2328140-37-8 30195-30-3
Synonym
Ro 24-7429; Ro-24-7429; Ro247429; Ro247429; Ro-247429; Ro 247429;
IUPAC/Chemical Name
3H-1,4-Benzodiazepin-2-amine, 7-chloro-N-methyl-5-(1H-pyrrol-2-yl)-
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)
SMILES Code
CNC1=NC2=CC=C(Cl)C=C2C(C3=CC=CN3)=NC1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
Ro 19-4603 is a benzodiazepine inverse agonist. It binds with high affinity to both diazepam-sensitive (DS) and diazepam-insensitive (DI) GABAA receptors (Ki values are ~ 0.2 and ~ 2.6 nM, respectively). Ro 19-4603 antagonizes effects of ethanol on locomotor behavior and suppresses ethanol intake in alcohol-preferring rats.
In vitro activity:
Ro 24-7429 also induced apoptosis and inhibited antigen-induced lymphocyte proliferation. Reference: Cell Immunol. 1996 Apr 10;169(1):40-6. https://pubmed.ncbi.nlm.nih.gov/8612292/
In vivo activity:
In this study, Ro 24-7429 treatment showed no evidence of antiviral activity against HIV. Nucleoside-treated patients had a mean 0.66 log10 reduction in infectious peripheral blood mononuclear cells, while Ro 24-7429 recipients had a mean 0.02 log10 reduction (P = 0.02). No dose-response relationships were observed in the Ro 24-7429 groups. Reference: The AIDS Clinical Trials Group 213 Team. J Infect Dis. 1995 Nov;172(5):1246-52. https://pubmed.ncbi.nlm.nih.gov/7594660/
Solvent mg/mL mM
Solubility
DMSO 62.5 229.16
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 272.74 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Patki AH, Lederman MM. HIV-1 Tat protein and its inhibitor Ro 24-7429 inhibit lymphocyte proliferation and induce apoptosis in peripheral blood mononuclear cells from healthy donors. Cell Immunol. 1996 Apr 10;169(1):40-6. doi: 10.1006/cimm.1996.0088. PMID: 8612292. 2. Cupelli LA, Hsu MC. The human immunodeficiency virus type 1 Tat antagonist, Ro 5-3335, predominantly inhibits transcription initiation from the viral promoter. J Virol. 1995 Apr;69(4):2640-3. doi: 10.1128/JVI.69.4.2640-2643.1995. PMID: 7884917; PMCID: PMC188946. 3. Haubrich RH, Flexner C, Lederman MM, Hirsch M, Pettinelli CP, Ginsberg R, Lietman P, Hamzeh FM, Spector SA, Richman DD. A randomized trial of the activity and safety of Ro 24-7429 (Tat antagonist) versus nucleoside for human immunodeficiency virus infection. The AIDS Clinical Trials Group 213 Team. J Infect Dis. 1995 Nov;172(5):1246-52. doi: 10.1093/infdis/172.5.1246. PMID: 7594660.
In vitro protocol:
1. Patki AH, Lederman MM. HIV-1 Tat protein and its inhibitor Ro 24-7429 inhibit lymphocyte proliferation and induce apoptosis in peripheral blood mononuclear cells from healthy donors. Cell Immunol. 1996 Apr 10;169(1):40-6. doi: 10.1006/cimm.1996.0088. PMID: 8612292. 2. Cupelli LA, Hsu MC. The human immunodeficiency virus type 1 Tat antagonist, Ro 5-3335, predominantly inhibits transcription initiation from the viral promoter. J Virol. 1995 Apr;69(4):2640-3. doi: 10.1128/JVI.69.4.2640-2643.1995. PMID: 7884917; PMCID: PMC188946.
In vivo protocol:
1. Haubrich RH, Flexner C, Lederman MM, Hirsch M, Pettinelli CP, Ginsberg R, Lietman P, Hamzeh FM, Spector SA, Richman DD. A randomized trial of the activity and safety of Ro 24-7429 (Tat antagonist) versus nucleoside for human immunodeficiency virus infection. The AIDS Clinical Trials Group 213 Team. J Infect Dis. 1995 Nov;172(5):1246-52. doi: 10.1093/infdis/172.5.1246. PMID: 7594660.
1: Haubrich RH, Flexner C, Lederman MM, Hirsch M, Pettinelli CP, Ginsberg R, Lietman P, Hamzeh FM, Spector SA, Richman DD. A randomized trial of the activity and safety of Ro 24-7429 (Tat antagonist) versus nucleoside for human immunodeficiency virus infection. The AIDS Clinical Trials Group 213 Team. J Infect Dis. 1995 Nov;172(5):1246-52. doi: 10.1093/infdis/172.5.1246. PMID: 7594660. 2: Dunne AL, Siregar H, Mills J, Crowe SM. HIV replication in chronically infected macrophages is not inhibited by the Tat inhibitors Ro-5-3335 and Ro-24-7429. J Leukoc Biol. 1994 Sep;56(3):369-73. doi: 10.1002/jlb.56.3.369. PMID: 8083610. 3: Patki AH, Lederman MM. HIV-1 Tat protein and its inhibitor Ro 24-7429 inhibit lymphocyte proliferation and induce apoptosis in peripheral blood mononuclear cells from healthy donors. Cell Immunol. 1996 Apr 10;169(1):40-6. doi: 10.1006/cimm.1996.0088. PMID: 8612292. 4: Braddock M, Cannon P, Muckenthaler M, Kingsman AJ, Kingsman SM. Inhibition of human immunodeficiency virus type 1 Tat-dependent activation of translation in Xenopus oocytes by the benzodiazepine Ro24-7429 requires trans-activation response element loop sequences. J Virol. 1994 Jan;68(1):25-33. doi: 10.1128/JVI.68.1.25-33.1994. PMID: 8254735; PMCID: PMC236260. 5: Luznik L, Kraus G, Guatelli J, Richman D, Wong-Staal F. Tat-independent replication of human immunodeficiency viruses. J Clin Invest. 1995 Jan;95(1):328-32. doi: 10.1172/JCI117660. PMID: 7814633; PMCID: PMC295435. 6: Biswas DK, Tius MA, Zhuo J, Pardee AB. Canventol inhibits HIV-1 replication by Tat-induced Tar-independent mechanism. J Acquir Immune Defic Syndr Hum Retrovirol. 1996 Jun 1;12(2):120-7. doi: 10.1097/00042560-199606010-00004. PMID: 8680882. 7: Hsu MC, Dhingra U, Earley JV, Holly M, Keith D, Nalin CM, Richou AR, Schutt AD, Tam SY, Potash MJ, et al. Inhibition of type 1 human immunodeficiency virus replication by a tat antagonist to which the virus remains sensitive after prolonged exposure in vitro. Proc Natl Acad Sci U S A. 1993 Jul 15;90(14):6395-9. doi: 10.1073/pnas.90.14.6395. PMID: 8341644; PMCID: PMC46938. 8: Cupelli LA, Hsu MC. The human immunodeficiency virus type 1 Tat antagonist, Ro 5-3335, predominantly inhibits transcription initiation from the viral promoter. J Virol. 1995 Apr;69(4):2640-3. doi: 10.1128/JVI.69.4.2640-2643.1995. PMID: 7884917; PMCID: PMC188946. 9: Biswas DK, Ahlers CM, Dezube BJ, Pardee AB. Cooperative inhibition of NF- kappa B and Tat-induced superactivation of human immunodeficiency virus type 1 long terminal repeat. Proc Natl Acad Sci U S A. 1993 Dec 1;90(23):11044-8. doi: 10.1073/pnas.90.23.11044. PMID: 8248210; PMCID: PMC47918. 10: Connell EV, Hsu MC, Richman DD. Combinative interactions of a human immunodeficiency virus (HIV) Tat antagonist with HIV reverse transcriptase inhibitors and an HIV protease inhibitor. Antimicrob Agents Chemother. 1994 Feb;38(2):348-52. doi: 10.1128/AAC.38.2.348. PMID: 7514858; PMCID: PMC284453. 11: Li CJ, Wang C, Pardee AB. Camptothecin inhibits Tat-mediated transactivation of type 1 human immunodeficiency virus. J Biol Chem. 1994 Mar 11;269(10):7051-4. PMID: 8125909. 12: Ehret A, Westendorp MO, Herr I, Debatin KM, Heeney JL, Frank R, Krammer PH. Resistance of chimpanzee T cells to human immunodeficiency virus type 1 Tat- enhanced oxidative stress and apoptosis. J Virol. 1996 Sep;70(9):6502-7. doi: 10.1128/JVI.70.9.6502-6507.1996. PMID: 8709290; PMCID: PMC190688. 13: Kira T, Hashimoto K, Baba M, Okamoto T, Shigeta S. 2-Glycineamide-5-chlorophenyl 2-pyrryl ketone, a non-benzodiazepin Tat antagonist, is effective against acute and chronic HIV-1 infections in vitro. Antiviral Res. 1996 Oct;32(2):55-62. doi: 10.1016/0166-3542(95)00980-9. PMID: 8891164. 14: Margalith M, Medina DJ, Hsiung GD, Smith BR, D'Aquila RT, Kaplan JC, Bechtel L, Wang MZ, Skolnik PR, Hirsch MS. Interactions between HIV-1 and cytomegalovirus in human osteosarcoma cells carrying both viruses. AIDS Res Hum Retroviruses. 1993 Jun;9(6):519-27. doi: 10.1089/aid.1993.9.519. PMID: 8394095. 15: Mhashilkar AM, Biswas DK, LaVecchio J, Pardee AB, Marasco WA. Inhibition of human immunodeficiency virus type 1 replication in vitro by a novel combination of anti-Tat single-chain intrabodies and NF-kappa B antagonists. J Virol. 1997 Sep;71(9):6486-94. doi: 10.1128/JVI.71.9.6486-6494.1997. PMID: 9261367; PMCID: PMC191923. 16: Germinario RJ, Colby-Germinario SP, Acel A, Chandok R, Davison K, Mak J, Kleiman L, Faust E, Wainberg MA. Effect of insulin-like growth factor I on HIV type 1 long terminal repeat-driven chloramphenicol acetyltransferase expression. AIDS Res Hum Retroviruses. 1999 Jun 10;15(9):829-36. doi: 10.1089/088922299310737. PMID: 10381171. 17: Maehr H, Zenchoff G, Coffen DL. An alternate synthesis of the Tat-antagonist 7-chloro-N-methyl-5-(1H-pyrrol-2-yl)-3H-1,4-benzodiazepin-2-amine. Bioorg Med Chem. 1995 Apr;3(4):391-5. doi: 10.1016/0968-0896(95)00026-d. PMID: 8581422. 18: Camsonne R, Bigot MC, Fusibet H, Moulin MA. Potentiel thérapeutique du Ro 5-3335. Une nouvelle benzodiazépine active in vitro contre les virus HIV-1 résistants ou non à l'AZT [Therapeutic potential of Ro 5-3335. New active benzodiazepine in vitro against HIV-1 viruses resistant or non-resistant to AZT]. Therapie. 1993 Mar-Apr;48(2):105-7. French. Erratum in: Therapie 1993 May- Jun;48(3):280. PMID: 8351676. 19: Turnabout on AIDS drug. Science. 1992 Jan 10;255(5041):154. PMID: 1553539. 20: New AIDS drug poised to move into development. Science. 1991 Dec 20;254(5039):1715. PMID: 1763318.
O'Hare M, Amarnani D, Whitmore HAB, An M, Marino C, Ramos L, Delgado-Tirado S, Hu X, Chmielewska N, Chandrahas A, Fitzek A, Heinrich F, Steurer S, Ondruschka B, Glatzel M, Krasemann S, Sepulveda-Falla D, Lagares D, Pedron J, Bushweller JH, Liu P, Arboleda-Velasquez JF, Kim LA. Targeting RUNX1 prevents pulmonary fibrosis and reduces expression of SARS-CoV-2 host mediators. Am J Pathol. 2021 Apr 21:S0002-9440(21)00161-9. doi: 10.1016/j.ajpath.2021.04.006. Epub ahead of print. PMID: 33894177; PMCID: PMC8059259.