| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
The inhibitor of mixed lymphocyte reaction (MLR) responses is DZ2002 (0.1, 1, 10 µM; 96 hours) [1]. DZ2002 (0.1, 1, 10 µM; 24 hours) prevents human THP-1 cells and mouse peritoneal exudate cells from producing TNF-α and IL-12 [1]. On differentiated THP-1 cells, DZ2002 (0.1, 1, 10 µM; 64 hours) inhibits B7 (CD80/CD86) expression [1].
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| ln Vivo |
The DNFB-induced DTH response is blocked by DZ2002 (2, 10, 50 mg/kg; intraperitoneal injection; twice). (DNFB-induced DTH is a Th1 cell-mediated immunological response; macrophages have been demonstrated to play a significant part in this process and IL-12 is significantly produced) [1]. DZ2002 (0.08, 2 mg/kg; intraperitoneal injection; once daily for 7 days) substantially reduces the production of antibodies and delayed-type hypersensitivity reactions [1]. In SSc mice models, DZ2002 (50, 100 mg/kg; oral; once daily for 4 weeks) effectively inhibits the formation of collagen, promotes its breakdown, and controls the expression of many soluble factors. Fibrosis [2].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: BALB/c and C57BL/6 splenocytes (mitomycin C pre-treated; mixed lymphocytes) Tested Concentrations: 0.1, 1, 10 µM Incubation Duration: 96 hrs (hours) Experimental Results: MLR inhibition 24.5, 42.3 and 46.0% at doses of 0.1, 1 and 10 µM respectively. Cell viability assay[1] Cell Types: TG-stimulated mouse peritoneal macrophages and human THP-1 cells Tested Concentrations: 0.1, 1, 10 µM Incubation Duration: 24 hrs (hours) Experimental Results: Significant blocking of approximately 1800 pg/mL of IL -12 p40 production in untreated cells dropped to approximately 850 pg/ml at 10 µM and Dramatically diminished the active p70 form in untreated cells from approximately 1200 pg/mL to approximately 50 pg/mL. TNF-α levels were diminished by 45%. Cell viability assay[1] Cell Types: THP-1 Cell Tested Concentrations: 0.1, 1, 10 µM Incubation Duration: 64 hrs (hours) Experimental Results: CD80, especially CD86 expression was Dramatically downregulated in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Male and female BALB/c and C57BL/6 mice (6 to 8 weeks old; DNFB-induced ear swelling model) [1].
Doses: 2, 10, 50 mg/kg Route of Administration: intraperitoneal (ip) injection; twice (1 hour before challenge and 24 hrs (hrs (hours)) after challenge) Experimental Results: Ear swelling was suppressed by 19.1%, 28.7% and 33.1%, respectively, in a dose-dependent manner . Animal/Disease Models: Male and female BALB/c and C57BL/6 mice (6 to 8 weeks old; DNFB-induced ear swelling model) [1]. Doses: 0.08, 2 mg/kg Route of Administration: intraperitoneal (ip) injection; single dose per day for 7 days. Experimental Results: Doses of 0.08 mg/kg and 2 mg/kg inhibited hemolysis by 24.5% and 18.4%, respectively, thereby reducing the production of anti-SRBC antibodies in the body. Animal/Disease Models: Wild-type C57BL/6 mice (8 to 12 weeks old; BLM-induced SSc mouse model) [2]. Doses: 50, 100 mg/kg Route of Administration: po (oral gavage); one time/day for 4 weeks. Experimental Results: BLM induced significant reductions in skin thickness and dermal thickness in mice. Dramatically diminished co |
| References |
[1]. Wu QL, et al. Inhibition of S-adenosyl-L-homocysteine hydrolase induces immunosuppression. J Pharmacol Exp Ther. 2005 May;313(2):705-11.
[2]. Zhang Z, et al. DZ2002 ameliorates fibrosis, inflammation, and vasculopathy in experimental systemic sclerosis models. Arthritis Res Ther. 2019 Dec 16;21(1):290. |
| Molecular Formula |
C10H13N5O3
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|---|---|
| Molecular Weight |
251.2419
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| Exact Mass |
251.102
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| CAS # |
33231-14-0
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| PubChem CID |
11658872
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| Appearance |
White to off-white solid powder
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| LogP |
-0.5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
18
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| Complexity |
303
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O([H])C([H])(C(=O)OC([H])([H])[H])C([H])([H])C([H])([H])N1C([H])=NC2=C(N([H])[H])N=C([H])N=C12
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| InChi Key |
HNKGMGPCSSJYOT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H13N5O3/c1-18-10(17)6(16)2-3-15-5-14-7-8(11)12-4-13-9(7)15/h4-6,16H,2-3H2,1H3,(H2,11,12,13)
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| Chemical Name |
methyl 4-(6-aminopurin-9-yl)-2-hydroxybutanoate
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ≥ 61 mg/mL (~242.80 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.95 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9803 mL | 19.9013 mL | 39.8026 mL | |
| 5 mM | 0.7961 mL | 3.9803 mL | 7.9605 mL | |
| 10 mM | 0.3980 mL | 1.9901 mL | 3.9803 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.
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