Pyrimethamine - 半岛电竞官方网址

Molecular Weight (MW)	248.71
Formula	C12H13ClN4
CAS No.	58-14-0
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility(In vitro)	DMSO: 10 mg/mL (40.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info	Chemical Name: 5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine InChi Key: WKSAUQYGYAYLPV-UHFFFAOYSA-N InChi Code: InChI=1S/C12H13ClN4/c1-2-9-10(11(14)17-12(15)16-9)7-3-5-8(13)6-4-7/h3-6H,2H2,1H3,(H4,14,15,16,17) SMILES Code: CCC1=C(C(=NC(=N1)N)N)C2=CC=C(C=C2)Cl
Synonyms	Malocid; Khloridin; BW 50-63; NCI-C01683; BW-50-63; BW50-63; Daraprim; NSC 3061; Tindurin; WR 297; Chloridine; Ethylpyrimidine; Chloridin; Daraprim; Pirimecidan; Malocide; Pirimetamin; RP 4753; Tindurine

Molecular Weight (MW)

248.71

Formula

C12H13ClN4

CAS No.

58-14-0

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility(In vitro)

DMSO: 10 mg/mL (40.2 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Other info

Chemical Name: 5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine

InChi Key: WKSAUQYGYAYLPV-UHFFFAOYSA-N

InChi Code: InChI=1S/C12H13ClN4/c1-2-9-10(11(14)17-12(15)16-9)7-3-5-8(13)6-4-7/h3-6H,2H2,1H3,(H4,14,15,16,17)

SMILES Code: CCC1=C(C(=NC(=N1)N)N)C2=CC=C(C=C2)Cl

Synonyms

Malocid; Khloridin; BW 50-63; NCI-C01683; BW-50-63; BW50-63; Daraprim; NSC 3061; Tindurin; WR 297; Chloridine; Ethylpyrimidine; Chloridin; Daraprim; Pirimecidan; Malocide; Pirimetamin; RP 4753; Tindurine

In Vitro	In vitroactivity: Pyrimethamine has an IC50 of 5–13 μM for the Hex isozymes at pH 4.3. Pyrimethamine increases the enzyme activity and protein level of the α and β subunits of Hex A in the βR505Q/Δ16kb cell line. Pyrimethamine-sulfadoxine is an inhibitor of dihydrofolate reductase(DHFR) that has been widely used to treat chloroquine-resistant Plasmodium falciparum malaria. Pyrimethamine is a potent inhibitor of mouse (m)Mate1 (K(i) = 145 nM) among renal organic cation transporters mOctn1 and mOctn2 (K(i)> 30 mM), mOct1 (K(i) = 3.6 mM), and mOct2 (K(i) = 6.0 mM). Pyrimethamine inhibits the uptake of metformin by kidney brush-border membrane vesicles (BBMVs) (K(i) = 41 nM) and canalicular membrane vesicles in the presence of outward gradient of H+. Pyrimethamine treatment significantly increases the kidney-to-plasma ratio of tetraethylammonium, and both the liver- and kidney-to-plasma ratios of metformin in mice, whereas it does not affect their plasma concentrations and urinary excretion rates. Pyrimethamine is a potent inhibitor of human (h)MATE1 and hMATE2-K (K(i) = 77 and 46 nM, respectively) and H+ and organic cation exchanger in human kidney BBMVs (K(i) = 31 nM) in the presence of outward gradient of H+. Cell Assay: In a PC12 cell-based assay, no compounds reduced SOD1 promoter activity without concomitant cytotoxicity. Additionally,pyrimethamine failed to repress levels of SOD1 protein in HeLa cells or homogenates of liver, spinal cord and brain of wild-type mice.
In Vivo	(131)I-Pyrimethamine (specific activity: 7.08 MBq/ mol) was injected intravenously into the tail vein of the control and infected rats. Static whole body images of the rats were acquired under the gamma camera at 5 min, 45 min, 2 h, 6 h, and 24 h following the intravenous administration of the radioactivity (3.7 MBq/rat). The 10-day treatment with 10mg/kg/day of fluconazole combined with 40/1mg/kg/day sulfadiazine and pyrimethamine resulted in 93% survival of CF1 mice acutely infected with the highly virulent T. gondii RH strain, versus 36% of mice treated with just sulfadiazine and pyrimethamine
Animal model	Rats
Formulation & Dosage	7.08 MBq/ mol; i.v.
References	J Biol Chem. 2007 Mar 23;282(12):9150-61; J Am Coll Cardiol. 2002 Aug 21;40(4):803-10.

In Vitro

In vitroactivity: Pyrimethamine has an IC50 of 5–13 μM for the Hex isozymes at pH 4.3. Pyrimethamine increases the enzyme activity and protein level of the α and β subunits of Hex A in the βR505Q/Δ16kb cell line. Pyrimethamine-sulfadoxine is an inhibitor of dihydrofolate reductase(DHFR) that has been widely used to treat chloroquine-resistant Plasmodium falciparum malaria. Pyrimethamine is a potent inhibitor of mouse (m)Mate1 (K(i) = 145 nM) among renal organic cation transporters mOctn1 and mOctn2 (K(i)> 30 mM), mOct1 (K(i) = 3.6 mM), and mOct2 (K(i) = 6.0 mM). Pyrimethamine inhibits the uptake of metformin by kidney brush-border membrane vesicles (BBMVs) (K(i) = 41 nM) and canalicular membrane vesicles in the presence of outward gradient of H+. Pyrimethamine treatment significantly increases the kidney-to-plasma ratio of tetraethylammonium, and both the liver- and kidney-to-plasma ratios of metformin in mice, whereas it does not affect their plasma concentrations and urinary excretion rates. Pyrimethamine is a potent inhibitor of human (h)MATE1 and hMATE2-K (K(i) = 77 and 46 nM, respectively) and H+ and organic cation exchanger in human kidney BBMVs (K(i) = 31 nM) in the presence of outward gradient of H+.

Cell Assay: In a PC12 cell-based assay, no compounds reduced SOD1 promoter activity without concomitant cytotoxicity. Additionally,pyrimethamine failed to repress levels of SOD1 protein in HeLa cells or homogenates of liver, spinal cord and brain of wild-type mice.

In Vivo

(131)I-Pyrimethamine (specific activity: 7.08 MBq/ mol) was injected intravenously into the tail vein of the control and infected rats. Static whole body images of the rats were acquired under the gamma camera at 5 min, 45 min, 2 h, 6 h, and 24 h following the intravenous administration of the radioactivity (3.7 MBq/rat). The 10-day treatment with 10mg/kg/day of fluconazole combined with 40/1mg/kg/day sulfadiazine and pyrimethamine resulted in 93% survival of CF1 mice acutely infected with the highly virulent T. gondii RH strain, versus 36% of mice treated with just sulfadiazine and pyrimethamine

Animal model

Rats

Formulation & Dosage

7.08 MBq/ mol; i.v.

References

J Biol Chem. 2007 Mar 23;282(12):9150-61; J Am Coll Cardiol. 2002 Aug 21;40(4):803-10.

CAS NO:	58-14-0
规格:	≥98%

包装	价格(元)
250mg	电议
500mg	电议
1g	电议
2g	电议
5g	电议