Allopurinol riboside |cas 16220-07-8

Cas No.:	16220-07-8
SMILES:	O[C@H]([C@@H]1O)[C@@H](O[C@@H]1CO)N(N=C2)C(N=CN3)=C2C3=O
Formula:	C₁₀H₁₂N₄O₅
M.Wt:	268.23
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Allopurinol-riboside competitively inhibits the action of purine nucleoside phosphorylase on inosine with a Ki of 277 μM. Lymphocyte blastogensis induced by PHA and Con A is significantly suppressed by allopurinol-riboside in a concentration-dependent manner. When LPS is used as a mitogen, the inhibition of allopurinol-ribosideon lymphocyte proliferation is less marked. Humoral immunity is not suppressed by allopurinol-riboside. Allopurinol riboside is an experimental agent for the treatment of leishmaniasis and American trypanosomiasis. Allopurinol riboside is effective against parasites, because a series of enzymes (analogous to those that mediate purine salvage in humans) convert it into 4-aminopyrazolopyrimidine ribonucleoside triphosphate, a cytotoxic product. Allopurinol riboside is selectively toxic, because it is not metabolized by the corresponding enzymes in humans.Allopurinol riboside peaks in plasma 1.6 hours after administration, has an elimination half-life of 3 hours, and steady-state concentrations in the therapeutic range. After oral administration, unexpectedly low levels of allopurinol riboside in plasma are attributable to incomplete absorption and rapid renal clearance. Probenecid reduces the renal clearance of allopurinol riboside, extends the half-life of allopurinol riboside in plasma, and triples the levels of allopurinol riboside in plasma.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47407	Antimalarial agent 3	Antimalarial agent 3 shows nanomolar antiplasmodial activity (IC50 = 0.035 μM) and has a very high selectivity index with respect to mammalian cells.
DC47406	Antileishmanial agent-2	Antileishmanial agent-2 shows submicromolar antileishmanial activity (IC50 = 0.29 μM) and a very high selectivity index with respect to mammalian cells.
DC47405	Antimalarial agent 2	Antimalarial agent 2 is a novel orally efficacious antimalarials that suggests a fast in vitro killing profile.
DC47404	TCMDC-125431	TCMDC-125431 is a novel disruptor of the malaria parasite calcium dynamics but minimally inhibits heme crystallization.
DC47403	TCMDC-136230	TCMDC-136230 is a novel disruptor of the malaria parasite calcium dynamics but minimally inhibits heme crystallization.
DC47402	TCMDC-125457	TCMDC-125457 is potent in inducing calcium redistribution but minimally inhibits heme crystallization. TCMDC-125457 demonstrated high efficacy when pulsed in a single-dose combination with artesunate against tightly synchronized artemisinin-resistant ring-stage parasites.
DC47401	Antileishmanial agent-1	Antileishmanial agent-1 exhibits the activity against L. amazonensis promastigotes (IC50 = 15.52 μM) and intracellular amastigotes (IC50 = 4.10 μM).
DC47400	BRD5018	BRD5018 is an antimalarial agent.
DC47399	MMV674850	MMV674850 is potent against asexual stage parasites at 2.7 and 4.5 nM and preferentially targets early-stage gametocytes (early-stage gametocyte: IC50 4.5 ± 3.6 nM; late-stage gametocyte: IC50 28.7 ± 0.2 nM).
DC47398	MMV666810	MMV666810, a 2-aminopyrazine similar to MMV390048, is potent against asexual parasites at 5.94 nM, but against gametocytes, it has a 3.3-fold selectivity to late-stage gametocytes compared to earlier stages (early-stage gametocyte: IC50 603 ± 88 nM; late-stage gametocyte: IC50 179 ± 8 nM).