ChemicalBook CAS DataBase List 33231-14-0

33231-14-0

Name	DZ-2002
CAS	33231-14-0
Molecular Formula	C10H13N5O3
MDL Number	MFCD28385844
Molecular Weight	251.25
MOL File	33231-14-0.mol

Chemical Properties

Boiling point	529.3±60.0 °C(Predicted)
density	1.58±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO: ≥ 61 mg/mL (242.80 mM)
form	Solid
pka	12.70±0.20(Predicted)
color	White to off-white

Hazard Information

Uses

DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis[1][2].

in vivo

DZ2002 (2, 10, 50 mg/kg; i.p.; twice) blocks the DNFB-induced DTH response. (DNFB-induced DTH is a Th1 cell-mediated immune response, in which IL-12 is highly expressed and macrophages have been shown to play an important role)^[1].
DZ2002 (0.08, 2 mg/kg; i.p.; single daily for 7 days) significantly suppresses a delayed-type hypersensitivity reaction as well as antibody secretion^[1].
DZ2002 (50, 100 mg/kg; p.o.; single daily for 4 weeks) exerts a potent anti-fibrotic effect on dermal fibrosis by reducing the production of collagen, facilitating its degradation and regulating expression of various soluble factors in SSc mice model^[2].

Animal Model:	Male and female BALB/c and C57BL/6 mice (6 to 8-week-old; DNFB-induced ear swelling model)^[1].
Dosage:	2, 10, 50 mg/kg
Administration:	Intraperitoneal injection; twice (1 h before and 24 h after challenge)
Result:	Suppressed ear swelling by 19.1, 28.7, and 33.1%, respectively and in a dose-dependent manner.

Animal Model:	Male and female BALB/c and C57BL/6 mice (6 to 8-week-old; DNFB-induced ear swelling model)^[1].
Dosage:	0.08, 2 mg/kg
Administration:	Intraperitoneal injection; single daily for 7 days.
Result:	Inhibited hemolysis by 24.5 and 18.4% at doses of 0.08 and 2 mg/kg, respectively, thus decreasing anti-SRBC antibody production in vivo.

Animal Model:	Wild-type C57BL/6 mice (8 to 12-week-old; BLM-induced mice model of SSc)^[2].
Dosage:	50, 100 mg/kg
Administration:	Oral gavage; single daily for 4 weeks.
Result:	Significantly decreased skin thickness and dermal thickness in BLM-induced mice. Significantly reduced collagen accumulation and α-SMA expression in the dermis of mice and suppressed the mRNA expression of vascular endothelial growth factor (VEGF) in mice skin tissue. Notably reduced collagen content and mRNA expression of the Col1a1 and Col1a2 while promoting that of the matrix metalloproteinase-13 (MMP-13) in the lesional skin of BLM-induced mice.

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. DOI:10.1124/jpet.104.080416
[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. DOI:10.1186/s13075-019-2074-9

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