2. Metabolic Enzyme/Protease Anti-infection
  3. Dihydrofolate reductase (DHFR) Parasite
  4. WR99210

WR99210  (Synonyms: BRL 6231 free base)

Cat. No.: HY-116387 Purity: 98.72%
COA Handling Instructions

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WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine (HY-18062)-resistant P. falciparum strains) as well as T. gondii.

For research use only. We do not sell to patients.

WR99210 Chemical Structure

WR99210 Chemical Structure

CAS No. : 47326-86-3

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Based on 2 publication(s) in Google Scholar

Other Forms of WR99210:

WR99210 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine (HY-18062)-resistant P. falciparum strains) as well as T. gondii[1][2][3].

IC50 & Target

IC50: <0.075 nM (DHFR)[3].
In Vitro

WR99210 (0-100 nM; 92 h) is highly effective against T. gondii tachyzoites in tissue culture[1].
WR99210 (0-100 nM; 92 h) shows low cytotoxicity to human foreskin fibroblasts[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

WR99210 Related Antibodies

Cell Viability Assay[1]

Cell Line: Human foreskin fibroblasts (T. gondii-infected)
Concentration: 0-100 nM
Incubation Time: 92 h
Result: Showed marked inhibition of T. gondii, with an IC50 value of approximately 50 nM.

Cell Cytotoxicity Assay[1]

Cell Line: Human foreskin fibroblasts
Concentration: 0-100 nM
Incubation Time: 92 h
Result: Lacked of toxicity for fibroblasts.
In Vivo

WR99210 (1.25 mg/kg; i.p.; single daily for 5 days) is highly effective against T. gondii tachyzoites in a mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male mice (T. gondii-infected)[1].
Dosage: 1.25 mg/kg
Administration: Intraperitoneal injection; single daily for 5 days.
Result: Exhibited intraperitoneal parasite numbers were 2 logs less in mice on the day 5.
Molecular Weight

394.68

Formula

C14H18Cl3N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1(N=C(N=C(N1OCCCOC2=C(C=C(C(Cl)=C2)Cl)Cl)N)N)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (12.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5337 mL 12.6685 mL 25.3370 mL
5 mM 0.5067 mL 2.5337 mL 5.0674 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.72%

COA (245 KB) LCMS (279 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5337 mL 12.6685 mL 25.3370 mL 63.3425 mL
5 mM 0.5067 mL 2.5337 mL 5.0674 mL 12.6685 mL
10 mM 0.2534 mL 1.2668 mL 2.5337 mL 6.3342 mL
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WR99210 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WR9921047326-86-3BRL 6231WR 99210WR-99210BRL6231BRL-6231Dihydrofolate reductase (DHFR)ParasiteP. falciparumparasitetoxoplasma gondiiT. gondiiInhibitorinhibitorinhibit

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