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Merck

SML3378

Sigma-Aldrich

Forodesine hydrochloride

≥98% (HPLC)

Sinónimos:

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

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About This Item

Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.21

Nivel de calidad

Ensayo

≥98% (HPLC)

Formulario

powder

condiciones de almacenamiento

desiccated

color

, White to very dark grey

solubilidad

DMSO: 2 mg/mL, clear

temp. de almacenamiento

−20°C

cadena SMILES

O=C1C2=C(NC=N1)C([C@@H]3N[C@@H]([C@H]([C@H]3O)O)CO)=CN2.Cl

Acciones bioquímicas o fisiológicas

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.

Pictogramas

Skull and crossbones

Palabra de señalización

Danger

Frases de peligro

Clasificaciones de peligro

Acute Tox. 3 Oral

Código de clase de almacenamiento

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


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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
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
R W Miles et al.
Biochemistry, 37(24), 8615-8621 (1998-06-24)
Genetic defects in human purine nucleoside phosphorylase cause T-cell deficiency as the major phenotype. It has been proposed that efficient inhibitors of the enzyme might intervene in disorders of T-cell function. Compounds with features of the transition-state structure of purine
Elisangela Oliveira Freitas et al.
PLoS neglected tropical diseases, 9(12), e0004297-e0004297 (2015-12-25)
Immucillins ImmA (IA), ImmH (IH) and SerMe-ImmH (SMIH) are synthetic deazapurine nucleoside analogues that inhibit Leishmania (L.) infantum chagasi and Leishmania (L.) amazonensis multiplication in vitro without macrophage toxicity. Immucillins are compared to the Glucantime standard drug in the chemotherapy

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