WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H333102
CAS#: 2772702-10-8 (HCl)
Description: Peldesine is a potent inhibitor of human CCRF-CEM T-cell proliferation. BCX-34 showed a complete inhibitory effect on the proliferation of T-cells in an in vitro system, whereas no influence was observed in B-cell lines. BCX-34 inhibits RBC PNP in vitro from humans, rats, and mice with IC50S ranging from 5 to 36 nM. BCX-34 also, in the presence but not in the absence of deoxyguanosine, inhibits human CCRF-CEM T-cell proliferation with an IC50 of 0.57 microM but not rat or mouse T-cell proliferation up to 30 microM. Inhibition of human T-cell proliferation is accompanied by an accumulation of intracellular dGTP with an associated reduction in GTP. BCX-34 may be useful in treating human T-cell proliferative inflammatory disorders.
Hodoodo Cat#: H333102
Name: Peldesine HCl
CAS#: 2772702-10-8 (HCl)
Chemical Formula: C12H13Cl2N5O
Exact Mass: 0.00
Molecular Weight: 314.170
Elemental Analysis: C, 45.88; H, 4.17; Cl, 22.57; N, 22.29; O, 5.09
Related CAS #: 2772702-10-8 (HCl) 133432-71-0 (free base)
Synonym: Peldesine HCl; BCX-34; BCX34; BCX 34;
IUPAC/Chemical Name: 4H-Pyrrolo(3,2-d)pyrimidin-4-one, 2-amino-3,5-dihydro-7-(3-pyridinylmethyl)- dihydrochloride
InChi Key: HQJPQOLISXXDRJ-UHFFFAOYSA-N
InChi Code: InChI=1S/C12H11N5O.2ClH/c13-12-16-9-8(4-7-2-1-3-14-5-7)6-15-10(9)11(18)17-12;;/h1-3,5-6,15H,4H2,(H3,13,16,17,18);2*1H
SMILES Code: O=C1C(NC=C2CC3=CC=CN=C3)=C2N=C(N)N1.[H]Cl.[H]Cl
Appearance: To be determined
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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:
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The following data is based on the product molecular weight 314.17 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.
| 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: | |
| In vitro protocol: | |
| In vivo protocol: |
1: El-Gazzar MGM, Ghorab MM, Amin MA, Korany M, Khedr MA, El-Gazzar MG, Sakr TM. Computational, in vitro and radiation-based in vivo studies on acetamide quinazolinone derivatives as new proposed purine nucleoside phosphorylase inhibitors for breast cancer. Eur J Med Chem. 2023 Feb 15;248:115087. doi: 10.1016/j.ejmech.2023.115087. Epub 2023 Jan 2. PMID: 36610250.
2: Wennberg E, Richards PQ, Bain PA, Huang V, Sullivan SD, Maverakis EM, Molina GE, Wu PA. Topical treatments for early-stage mycosis fungoides using Grading Recommendations Assessment, Development and Evaluation (GRADE) criteria: A systematic review. JAAD Int. 2021 Mar 11;3:26-41. doi: 10.1016/j.jdin.2021.01.002. PMID: 34409369; PMCID: PMC8362313.
3: Valipour A, Jäger M, Wu P, Schmitt J, Bunch C, Weberschock T. Interventions for mycosis fungoides. Cochrane Database Syst Rev. 2020 Jul 7;7(7):CD008946. doi: 10.1002/14651858.CD008946.pub3. PMID: 32632956; PMCID: PMC7389258.
4: Wu PA, Huang V, Bigby ME. Interventions for mycosis fungoides: critical commentary on a Cochrane Systematic Review. Br J Dermatol. 2014 May;170(5):1015-20. doi: 10.1111/bjd.12954. PMID: 24841586.
5: Weberschock T, Strametz R, Lorenz M, Röllig C, Bunch C, Bauer A, Schmitt J. Interventions for mycosis fungoides. Cochrane Database Syst Rev. 2012 Sep 12;(9):CD008946. doi: 10.1002/14651858.CD008946.pub2. Update in: Cochrane Database Syst Rev. 2020 Jul 7;7:CD008946. PMID: 22972128.
6: Maloney DM. Case study: institutional review board (IRB) did not know about subject problem until after study. Hum Res Rep. 2006 May;21(5):6-7. PMID: 16832916.
7: Patterson TJ, Ngo M, Aronov PA, Reznikova TV, Green PG, Rice RH. Biological activity of inorganic arsenic and antimony reflects oxidation state in cultured human keratinocytes. Chem Res Toxicol. 2003 Dec;16(12):1624-31. doi: 10.1021/tx034146y. PMID: 14680377.
8: Foss FM. An oncologist's approach to therapy for cutaneous T-cell lymphoma. Clin Lymphoma. 2000 Nov;1 Suppl 1:S9-14. doi: 10.3816/clm.2000.s.002. PMID: 11707857.
9: Duvic M, Olsen EA, Omura GA, Maize JC, Vonderheid EC, Elmets CA, Shupack JL, Demierre MF, Kuzel TM, Sanders DY. A phase III, randomized, double-blind, placebo-controlled study of peldesine (BCX-34) cream as topical therapy for cutaneous T-cell lymphoma. J Am Acad Dermatol. 2001 Jun;44(6):940-7. doi: 10.1067/mjd.2001.113478. PMID: 11369904.
10: Viegas TX, Van Winkle LL, Lehman PA, Franz SF, Franz TJ. Evaluation of creams and ointments as suitable formulations for peldesine. Int J Pharm. 2001 May 21;219(1-2):73-80. doi: 10.1016/s0378-5173(01)00632-9. PMID: 11337167.
11: Viegas TX, Van Winkle LL. Preformulation studies for the development of a parenteral liquid formulation of the immunomodulator, peldesine. PDA J Pharm Sci Technol. 1999 Nov-Dec;53(6):303-8. PMID: 10754728.
12: Morris PE Jr, Omura GA. Inhibitors of the enzyme purine nucleoside phosphorylase as potential therapy for psoriasis. Curr Pharm Des. 2000 Jun;6(9):943-59. doi: 10.2174/1381612003400083. PMID: 10828318.
13: Viegas TX, Omura GA, Stoltz RR, Kisicki J. Pharmacokinetics and pharmacodynamics of peldesine (BCX-34), a purine nucleoside phosphorylase inhibitor, following single and multiple oral doses in healthy volunteers. J Clin Pharmacol. 2000 Apr;40(4):410-20. doi: 10.1177/00912700022008991. Erratum in: J Clin Pharmacol 2000 Jun;40(6):664. PMID: 10761169.
14: Litsky ML, Hohl CM, Lucas JH, Jurkowitz MS. Inosine and guanosine preserve neuronal and glial cell viability in mouse spinal cord cultures during chemical hypoxia. Brain Res. 1999 Mar 13;821(2):426-32. doi: 10.1016/s0006-8993(99)01086-0. PMID: 10064830.
15: Conry RM, Bantia S, Turner HS, Barlow DL, Allen KO, LoBuglio AF, Montgomery JA, Walsh GM. Effects of a novel purine nucleoside phosphorylase inhibitor, BCX-34, on activation and proliferation of normal human lymphoid cells. Immunopharmacology. 1998 Jul;40(1):1-9. doi: 10.1016/s0162-3109(98)00012-5. PMID: 9776473.
16: Iwata H, Wada Y, Walsh M, Montgomery JA, Hirose H, Mendez R, Cicciarelli J, Iwaki Y. In vitro study of BCX-34: a new human T-lymphocyte-specific purine phosphorylase inhibitor. Transplant Proc. 1998 Jun;30(4):983-6. doi: 10.1016/s0041-1345(98)00119-5. PMID: 9636397.
17: Yan J, Lu Z, Walsh GM, Wheeler RH, Diasio RB. High-performance liquid chromatographic determination of 9-(3-pyridylmethyl)-9-deazaguanine (BCX-34) in biological fluids. J Chromatogr B Biomed Sci Appl. 1997 Mar 7;690(1-2):295-303. doi: 10.1016/s0378-4347(96)00365-9. PMID: 9106056.
18: Bantia S, Montgomery JA, Johnson HG, Walsh GM. In vivo and in vitro pharmacologic activity of the purine nucleoside phosphorylase inhibitor BCX-34: the role of GTP and dGTP. Immunopharmacology. 1996 Oct;35(1):53-63. doi: 10.1016/0162-3109(96)00123-3. PMID: 8913795.
19: Wada Y, Yagihashi A, Terasawa K, Miyao N, Hirata K, Cicciarelli J, Iwaki Y. BCX-34: a novel T-cell selective immunosuppressant: purine nucleoside phosphorylase (PNP) inhibitor. Artif Organs. 1996 Aug;20(8):849-52. doi: 10.1111/j.1525-1594.1996.tb04557.x. PMID: 8853794.
