2. GPCR/G Protein Apoptosis
  3. Guanylate Cyclase Apoptosis
  4. Praliciguat

Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase (sGC) activator. Praliciguat can increases cGMP via the nitric oxide (NO)-sGC pathway. Praliciguat can inhibit the expression of proinflammatory cytokines and inhibit apoptosis. Praliciguat can promote vasodilation. Praliciguat can be used for the researches of metabolic disease and cardiovascular disease, such as hypertension, diabetes and heart failure.

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Praliciguat

Praliciguat 화학구조

CAS No. : 1628730-49-3

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 2 publication(s) in Google Scholar

Other Forms of Praliciguat:

Praliciguat Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase (sGC) activator. Praliciguat can increases cGMP via the nitric oxide (NO)-sGC pathway. Praliciguat can inhibit the expression of proinflammatory cytokines and inhibit apoptosis. Praliciguat can promote vasodilation. Praliciguat can be used for the researches of metabolic disease and cardiovascular disease, such as hypertension, diabetes and heart failure[1][2][3].

IC50 & Target

EC50: 197 nM (sGC)[1]
In Vitro

Praliciguat stimulates soluble guanylate cyclase in HEK-293 cells with an EC50 of 197 nM[1].
Praliciguat demonstrates concentration-dependent relaxation of pre-contracted subcutaneous resistance arteries (EC50 = 34.7 nM)[1].
Praliciguat (10 μM, 48 h) inhibits the expression of proinflammatory cytokines and secretion of monocyte chemoattractant protein 1 in TNF-α-challenged proximal tubular epithelial cells (RPTC)[2].
Praliciguat (1-10 μM, 48 h) inhibits TGF-β-mediated apoptosis in RPTC[2].

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

Praliciguat Related Antibodies
In Vivo

Praliciguat (1 mg/kg, p.o.) reduces arterial pressure (MAP) in normotensive and hypertensive rats[1].
Praliciguat (1-10 mg/kg, p.o.) attenuates proteinuria in obese ZSF1 rats model of diabetic nephropathy[2].
Praliciguat (1-10 mg/kg, p.o., daily for 2-7 weeks) attenuates inflammation, fibrosis, and end-organ damage in the Dahl rats model of cardiorenal failure[3].

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

Animal Model: Obese ZSF1 rat model of diabetic nephropathy [2]
Dosage: 1, 3 and 10 mg/kg
Administration: Orally administration
Result: Attenuated proteinuria.
Reduced fasting glucose and cholesterol.
Animal Model: Dahl rats model of cardiorenal failure[3]
Dosage: 1, 3 and 10 mg/kg
Administration: Orally administration
Result: Reduced blood pressure.
Improved cardiorenal damage, daily for 2-7 weeks.
Attenuated the increase in circulating markers of inflammation and fibrosis.
Clinical Trial
분자량

534.36

화학식

C21H14F8N6O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=C(C=CC=C1)CN2C(C3=NOC=C3)=CC(C4=NC=C(F)C(NCC(C(F)(F)F)(O)C(F)(F)F)=N4)=N2
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
용액&용해도
In Vitro: 

DMSO : 250 mg/mL (467.85 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 1.8714 mL 9.3570 mL 18.7140 mL
5 mM 0.3743 mL 1.8714 mL 3.7428 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.

  • 몰농도 계산기

  • 농도 희석 계산기

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:

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: ≥ 2.08 mg/mL (3.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.89 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 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)

g

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.
순도&문서
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8714 mL 9.3570 mL 18.7140 mL 46.7849 mL
5 mM 0.3743 mL 1.8714 mL 3.7428 mL 9.3570 mL
10 mM 0.1871 mL 0.9357 mL 1.8714 mL 4.6785 mL
15 mM 0.1248 mL 0.6238 mL 1.2476 mL 3.1190 mL
20 mM 0.0936 mL 0.4678 mL 0.9357 mL 2.3392 mL
25 mM 0.0749 mL 0.3743 mL 0.7486 mL 1.8714 mL
30 mM 0.0624 mL 0.3119 mL 0.6238 mL 1.5595 mL
40 mM 0.0468 mL 0.2339 mL 0.4678 mL 1.1696 mL
50 mM 0.0374 mL 0.1871 mL 0.3743 mL 0.9357 mL
60 mM 0.0312 mL 0.1559 mL 0.3119 mL 0.7797 mL
80 mM 0.0234 mL 0.1170 mL 0.2339 mL 0.5848 mL
100 mM 0.0187 mL 0.0936 mL 0.1871 mL 0.4678 mL
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Praliciguat 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:

Praliciguat1628730-49-3IW-1973IW1973IW 1973Guanylate CyclaseApoptosisGuanylate cyclaseNOCGMPHypertensionDiabetesHeart failureInhibitorinhibitorinhibit

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상품명:
Praliciguat
Cat. No.:
HY-109039
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