2. GPCR/G Protein
  3. P2Y Receptor
  4. NF157

NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA).

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NF157

NF157 화학구조

CAS No. : 104869-26-3

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
1 mg 해외재고보유
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg   견적 받기  
100 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

NF157 Related Antibodies

Top Publications Citing Use of Products

View All P2Y Receptor Isoform Specific Products:

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P2Y1 Receptor P2Y2 Receptor P2Y6 Receptor P2Y11 Receptor P2Y12 Receptor P2Y13 Receptor P2Y14 Receptor

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively[1]. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA)[2].

IC50 & Target

pKi: 7.35 (P2Y11)[1]
IC50: 463 nM (P2Y11), 1811 µM (P2Y1), 170 µM (P2Y2)[1]
Ki: 44.3 nM (P2Y11), 187 µM (P2Y1), 28.9 µM (P2Y2)[1]
In Vitro

NF157 displays selectivity for P2Y11 over P2Y1 (>650-fold), P2Y2 (>650-fold), P2X2 (3-fold), P2X3 (8-fold), P2X4 (>22-fold), and P2X7 (>67-fold) but no selectivity over P2X1[1].
NF157 (30 and 60 µM; 24 hours) causes a significant reduction in degradation of type II collagen in a dose-dependent manner. 60 µM NF157 nearly completely rescues type II collagen from degradation induced by TNF-α (10 ng/mL)[2].
NF157 (30 and 60 µM; 24 hours) almost fully restores nuclear translocation of p65 triggered by TNF-α (10 ng/mL) and significantly reduces the luciferase activity of NF-κB[2].

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

NF157 Related Antibodies

Western Blot Analysis[2]

Cell Line: SW1353 cells
Concentration: 30 and 60 µM
Incubation Time: 24 hours
Result: Ameliorated TNF-α-induced degradation of type II collagen.

Western Blot Analysis[2]

Cell Line: SW1353 cells
Concentration: 30 and 60 µM
Incubation Time: 24 hours
Result: Reduced TNF-α-induced activation of NF-κB.
분자량

1437.10

화학식

C49H28F2N6Na6O23S6
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

O=C(NC1=CC(C(NC2=CC(C(NC3=CC=C(S(=O)(O[Na])=O)C4=CC(S(=O)(O[Na])=O)=CC(S(=O)(O[Na])=O)=C34)=O)=CC=C2F)=O)=CC=C1)NC5=CC(C(NC6=CC(C(NC7=CC=C(S(=O)(O[Na])=O)C8=CC(S(=O)(O[Na])=O)=CC(S(=O)(O[Na])=O)=C78)=O)=CC=C6F)=O)=CC=C5
선적

Room temperature in continental US; may vary elsewhere.
보관

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

용액&용해도
In Vitro: 

DMSO : 33.33 mg/mL (23.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 1 mg/mL (0.70 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.6958 mL 3.4792 mL 6.9585 mL
5 mM 0.1392 mL 0.6958 mL 1.3917 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 (sealed storage, away from moisture). 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:

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (1.74 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 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (1.74 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)

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

Purity: 99.13%

SDS (252 KB)

COA (248 KB) HNMR (1368 KB) RP-HPLC (609 KB) MS (479 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 (sealed storage, away from moisture). 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
DMSO 1 mM 0.6958 mL 3.4792 mL 6.9585 mL 17.3961 mL
5 mM 0.1392 mL 0.6958 mL 1.3917 mL 3.4792 mL
10 mM 0.0696 mL 0.3479 mL 0.6958 mL 1.7396 mL
15 mM 0.0464 mL 0.2319 mL 0.4639 mL 1.1597 mL
20 mM 0.0348 mL 0.1740 mL 0.3479 mL 0.8698 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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NF157 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:

NF157104869-26-3NF 157NF-157P2Y ReceptorOsteoarthritisP2Y11matrixMMPcollagenaggrecanNF-κBInhibitorinhibitorinhibit

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상품명:
NF157
Cat. No.:
HY-108672
수량:
MCE Japan Authorized Agent:

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SAFETY DATA SHEET (SDS)

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