SML3378
Forodesine hydrochloride
≥98% (HPLC)
别名:
7-[(2S,3S,4R,5R)-3,4-Dihydroxy-5-(hydroxymethyl)-2-pyrrolidinyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one, hydrochloride salt, BCX-1777 HCl, ImmH HCl, Immucillin-H HCl
质量水平
方案
≥98% (HPLC)
表单
powder
储存条件
desiccated
颜色
, White to very dark grey
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
O=C1C2=C(NC=N1)C([C@@H]3N[C@@H]([C@H]([C@H]3O)O)CO)=CN2.Cl
相关类别
生化/生理作用
Forodesine (BCX-1777; ImmH; Immucillin-H) is an orally active, tight-binding (bovine/human PNP Ki = 23/72 pM) and highly potent purine nucleoside phosphorylase (PNP, PNPase) inhibtor (IC50 in nM = 0.48/mouse, 0.66/monkey, 1.19/human, 1.24/rat, 1.57/dog) that mimics the PNP transition-state structure. Forodesine inhibits human T-cell proliferation stimulated by IL-2, MLR- and PHA in cultures (IC50 in the presence of 10 μM dGuo = 60, 50, and 387 nM, respectively) and shows in vivo efficacy in a xenogeneic graft vs. host disease model using hu-PBL SCID mice (20 mg/kg b.i.d. p.o.).
Orally active, tight-binding and highly potent purine nucleoside phosphorylase (PNP; PNPase) transition-state inhibtor in vitro and in vivo.
警示用语：
Danger
危险声明
危险分类
Acute Tox. 3 Oral
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Liesbeth Bieghs et al.
Advances in hematology, 2010, 131895-131895 (2010-10-29)
Multiple myeloma (MM) is the second most commonly diagnosed hematological malignancy, characterized by a monoclonal proliferation of malignant cells in the bone marrow. Despite recent advances in treatment strategies, MM remains incurable and new therapeutical targets are needed. Recently forodesine
S Bantia et al.
International immunopharmacology, 1(6), 1199-1210 (2001-06-16)
Patients with purine nucleoside phosphorylase (PNP) deficiency present a selective T-cell immunodeficiency. Inhibitors of PNP are, therefore, of interest as potential T-cell selective immunosuppressive agents. BCX-1777 is a potent inhibitor of PNP from various species including human, mouse, rat, monkey
Tingting Wang et al.
Nature metabolism, 2(7), 635-647 (2020-07-23)
T cells undergo metabolic rewiring to meet their bioenergetic, biosynthetic and redox demands following antigen stimulation. To fulfil these needs, effector T cells must adapt to fluctuations in environmental nutrient levels at sites of infection and inflammation. Here, we show
Kumudha Balakrishnan et al.
Blood, 116(7), 1083-1091 (2010-05-06)
Forodesine, a purine nucleoside phosphorylase inhibitor, displays in vitro activity in chronic lymphocytic leukemia (CLL) cells in presence of dGuo, which is the basis for an ongoing clinical trial in patients with fludarabine-refractory CLL. Initial clinical data indicate forodesine has
Ke-Qi Fan et al.
Cell, 179(4), 864-879 (2019-11-02)
Physical or mental stress leads to neuroplasticity in the brain and increases the risk of depression and anxiety. Stress exposure causes the dysfunction of peripheral T lymphocytes. However, the pathological role and underlying regulatory mechanism of peripheral T lymphocytes in
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