2. Metabolic Enzyme/Protease
  3. Aminopeptidase
  4. Firibastat

Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats.

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Firibastat

Firibastat 화학구조

CAS No. : 648927-86-0

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in Water 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  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 1 publication(s) in Google Scholar

Other Forms of Firibastat:

Firibastat Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Firibastat

View All Aminopeptidase Isoform Specific Products:

View All Isoforms
CD13 LTA4H

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats[1][2].

In Vivo

When given orally, Firibastat (0.1-30 mg/kg; p.o.) crosses the gastrointestinal and blood-brain barriers, enters the brain, and generates two active molecules of EC33 which inhibit brain APA activity, blocking brain angiotensin III formation, and decrease blood pressure for several hours in hypertensive rats[2].

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

Animal Model: Normotensive and hypertensive DOCA-salt rats[1]
Dosage: 0.1-30 mg/kg
Administration: P.o.
Result: Resulting in a dose-dependent decrease in mean arterial blood pressure (MABP).
Clinical Trial
분자량

368.51

화학식

C8H20N2O6S4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(CC[C@H](N)CSSC[C@@H](N)CCS(=O)(O)=O)(O)=O
선적

Room temperature in continental US; may vary elsewhere.
보관
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
In Vitro: 

H2O : 25 mg/mL (67.84 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7136 mL 13.5682 mL 27.1363 mL
5 mM 0.5427 mL 2.7136 mL 5.4273 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (271.36 mM); Clear solution; Need ultrasonic

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
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
순도&문서

Purity: 98.0%

SDS (394 KB)

COA (245 KB) HNMR (235 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.7136 mL 13.5682 mL 27.1363 mL 67.8408 mL
5 mM 0.5427 mL 2.7136 mL 5.4273 mL 13.5682 mL
10 mM 0.2714 mL 1.3568 mL 2.7136 mL 6.7841 mL
15 mM 0.1809 mL 0.9045 mL 1.8091 mL 4.5227 mL
20 mM 0.1357 mL 0.6784 mL 1.3568 mL 3.3920 mL
25 mM 0.1085 mL 0.5427 mL 1.0855 mL 2.7136 mL
30 mM 0.0905 mL 0.4523 mL 0.9045 mL 2.2614 mL
40 mM 0.0678 mL 0.3392 mL 0.6784 mL 1.6960 mL
50 mM 0.0543 mL 0.2714 mL 0.5427 mL 1.3568 mL
60 mM 0.0452 mL 0.2261 mL 0.4523 mL 1.1307 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Firibastat 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:

Firibastat648927-86-0QGC001 RB150QGC 001QGC-001RB150RB 150RB-150Aminopeptidasefirst-in-classangiotensinbrainhypertensivebloodpressureInhibitorinhibitorinhibit

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상품명:
Firibastat
Cat. No.:
HY-109058
수량:
MCE Japan Authorized Agent:

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SAFETY DATA SHEET (SDS)

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