Canagliflozin hemihydrate (Synonyms: JNJ 28431754 hemihydrate)

Name: Canagliflozin hemihydrate
Brand: MedChemExpress
SKU: HY-I0383
Rating: 5.0 (46 reviews)

Cat. No.: HY-I0383 Pureza: 99.95%: Ficha de datos
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Canagliflozin hemihydrate (JNJ28431754 hemihydrate) is a selective SGLT2 inhibitor with IC₅₀s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.

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No. CAS : 928672-86-0

Tamaño	Stock	Cantidad

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
100 mg	En stock	Estimated Time of Arrival: December 31
500 mg	En stock	Estimated Time of Arrival: December 31
1 g	En stock	Estimated Time of Arrival: December 31
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Revisión del cliente

Based on 46 publication(s) in Google Scholar

Other Forms of Canagliflozin hemihydrate:

Canagliflozin In-stock

46 Publications Citing Use of MCE Canagliflozin hemihydrate

: Canagliflozin hemihydrate purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Dec;132:110821. [Abstract]; MCF-7 and ZR-75-1 cells are exposed to Canagliflozin 0, 11, 33, and 100 μM for 24 h and protein levels of p-AMPK, total AMPK, p-p70S6K1 and total p70S6K1 are detected using immunoblot assay.

: Canagliflozin hemihydrate purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Jun:152:45-59. [Abstract]; Effects of NF-κB inhibitor (10 μM MLN120B) is measured on p62 protein in LPS-induced RAW264.7 cells.

: Canagliflozin hemihydrate purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Jun:152:45-59. [Abstract]; PFK2 expression is significantly increased by LPS but is attenuated by Canagliflozin (CAN).

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Ver todos los productos específicos de isoformas SGLT:

Ver todas las isoformas

SGLT1 SGLT2

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Pureza y Documentación
Referencias
Revisión del cliente

Descripciòn

Canagliflozin hemihydrate (JNJ28431754 hemihydrate) is a selective SGLT2 inhibitor with IC₅₀s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively^[1].

IC₅₀ & Target

SGLT2

In Vitro

Canagliflozin inhibits Na⁺-dependent ¹⁴C-AMG uptake in CHO-hSGLT2 cells, with an IC₅₀ of 4.4±1.2 nM. Similar IC₅₀ values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC₅₀ = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits ¹⁴C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC₅₀ of 684±159 nM and >1,000 nM, respectively^[1].

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

In Vivo

Canagliflozin (30 mg/kg treatment for 4 weeks) reduces blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice^[1].
Canagliflozin (3 mg/kg for 3 weeks) increases urinary glucose excretion (UGE) with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight In ZF rats^[1].

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

Animal Model:	Diet-induced obese, insulin resistantmice (DIO) Mice^[1]
Dosage:	30 mg/kg
Administration:	Oral gavage; daily; 4 weeks
Result:	Reduced BG levels, respiratory exchange ratio, and body weight gain.

Animal Model:	Male Zucker fatty (ZF) obese, insulin resistant rats^[1]
Dosage:	3 mg/kg
Administration:	Oral gavage; daily; 3 weeks
Result:	UGE was increased with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight.

Ensayo clínico

Peso molecular

453.52

Fòrmula

C₂₄H₂₆FO_5.5S

No. CAS

928672-86-0

Appearance

Solid

Color

Off-white to yellow

SMILES

CC1=CC=C([C@H]2[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O2)C=C1CC3=CC=C(C4=CC=C(F)C=C4)S3.[0.5H2O]

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : ≥ 100 mg/mL (220.50 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2050 mL	11.0249 mL	22.0497 mL
5 mM	0.4410 mL	2.2050 mL	4.4099 mL
10 mM	0.2205 mL	1.1025 mL	2.2050 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureza y Documentación

Purity: 99.95%

Select Batch:

Ficha de datos (277 KB) SDS (393 KB)

COA (253 KB) HNMR (198 KB) RP-HPLC (345 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Liang Y, et al. Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models. PLoS One. 2012;7(2):e30555. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2050 mL	11.0249 mL	22.0497 mL	55.1244 mL
	5 mM	0.4410 mL	2.2050 mL	4.4099 mL	11.0249 mL
	10 mM	0.2205 mL	1.1025 mL	2.2050 mL	5.5124 mL
	15 mM	0.1470 mL	0.7350 mL	1.4700 mL	3.6750 mL
	20 mM	0.1102 mL	0.5512 mL	1.1025 mL	2.7562 mL
	25 mM	0.0882 mL	0.4410 mL	0.8820 mL	2.2050 mL
	30 mM	0.0735 mL	0.3675 mL	0.7350 mL	1.8375 mL
	40 mM	0.0551 mL	0.2756 mL	0.5512 mL	1.3781 mL
	50 mM	0.0441 mL	0.2205 mL	0.4410 mL	1.1025 mL
	60 mM	0.0367 mL	0.1837 mL	0.3675 mL	0.9187 mL
	80 mM	0.0276 mL	0.1378 mL	0.2756 mL	0.6891 mL
	100 mM	0.0220 mL	0.1102 mL	0.2205 mL	0.5512 mL

Canagliflozin hemihydrate 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:

Canagliflozin hemihydrate928672-86-0JNJ 28431754 hemihydrateSGLTSodium-dependent glucose cotransportersInhibitorinhibitorinhibit

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Canagliflozin hemihydrate (Synonyms: JNJ 28431754 hemihydrate)

Revisión del cliente

Other Forms of Canagliflozin hemihydrate:

Canagliflozin hemihydrate Related Antibodies

46 Publications Citing Use of MCE Canagliflozin hemihydrate

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas SGLT:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Canagliflozin hemihydrate Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Canagliflozin hemihydrate Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

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SAFETY DATA SHEET (SDS)

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