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%
SDS 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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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

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  • Purity & Documentation

  • References

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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].
Cellular Effect
Cell Line Type Value Description References
Vero IC50
> 1 μM
Compound: WR99210
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
[PMID: 32294614]
Vero IC50
> 10 μM
Compound: WR99210
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by SRB assay
[PMID: 34624822]
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%

SDS (252 KB)

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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