2. MAPK/ERK Pathway Autophagy
  3. p38 MAPK Autophagy
  4. Pamapimod

Pamapimod  (Synonyms: Ro4402257; R1503)

製品番号: HY-10405 純度: 99.71%
COA 取扱説明書 Technical Support

Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment.

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Pamapimod

Pamapimod 構造式

CAS 番号 : 449811-01-2

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 在庫あり
Solution
10 mM * 1 mL in DMSO USD 165 在庫あり
Solid
5 mg $150 在庫あり
10 mg $240 在庫あり
25 mg $480 在庫あり
50 mg $768 在庫あり
100 mg $1040 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

Other Forms of Pamapimod:

Pamapimod 関連抗体

Top Publications Citing Use of Products

p38 MAPK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment[1].

IC50 & Target[1]

p38α

14 nM (IC50)

p38α

1.3 nM (Ki)

p38β

480 (IC50)

p38β

120 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
> 30 μM
Compound: 5
Cytotoxicity against HEK293 after 24 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against HEK293 after 24 hrs by CellTiter-Glo luminescent cell viability assay
[PMID: 26704265]
THP-1 IC50
0.025 μM
Compound: 2b, Pamapimod
Inhibition of LPS-induced TNFalpha production in human THP1 cells after 2 hrs by ELISA
Inhibition of LPS-induced TNFalpha production in human THP1 cells after 2 hrs by ELISA
[PMID: 21375264]
THP-1 IC50
25 nM
Compound: 1
Inhibition of LPS-induced TNFalpha production in human THP1 cells by ELISA
Inhibition of LPS-induced TNFalpha production in human THP1 cells by ELISA
[PMID: 19950901]
体外実験

Pamapimod binds to JNK kinases with Ki values of 190 nM, 16 nM and 19 nM for Jnk1, Jnk2 and Jnk3, respectively[1].
After lipopolysaccharide (LPS) stimulation of the human myelomonocytic cell line (THP-1), secretion of TNF-α is inhibited by Pamapimod, with an EC50 of 25 nM. Pamapimod suppresses TNF-α and IL-1β production in whole blood, with EC50 values of 0.40 and 0.10 μM, respectively[1].

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

Pamapimod 関連抗体
体内実験

Pamapimod (0-150 mg/kg; oral gavage; once daily; DBA/1J female mice) treatment reduces inflammation and bone loss in murine collagen-induced arthritis[1].

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

Animal Model: DBA/1J female mice (8-10 weeks of age) induced murine collagen[1]
Dosage: 0 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg, 90 mg/kg, 150 mg/kg
Administration: Oral gavage; once daily
Result: Reduced inflammation and bone loss.
分子量

406.38

分子式

C19H20F2N4O4
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC(CCO)CCO)N=C3N1C
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 34 mg/mL (83.67 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 2.4608 mL 12.3038 mL 24.6075 mL
5 mM 0.4922 mL 2.4608 mL 4.9215 mL
10 mM 0.2461 mL 1.2304 mL 2.4608 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

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体積 （開始）

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション

純度: 99.71%

COA (247 KB) LCMS (101 KB)

取扱説明書 (2659 KB)
参考文献

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 2.4608 mL 12.3038 mL 24.6075 mL 61.5188 mL
5 mM 0.4922 mL 2.4608 mL 4.9215 mL 12.3038 mL
10 mM 0.2461 mL 1.2304 mL 2.4608 mL 6.1519 mL
15 mM 0.1641 mL 0.8203 mL 1.6405 mL 4.1013 mL
20 mM 0.1230 mL 0.6152 mL 1.2304 mL 3.0759 mL
25 mM 0.0984 mL 0.4922 mL 0.9843 mL 2.4608 mL
30 mM 0.0820 mL 0.4101 mL 0.8203 mL 2.0506 mL
40 mM 0.0615 mL 0.3076 mL 0.6152 mL 1.5380 mL
50 mM 0.0492 mL 0.2461 mL 0.4922 mL 1.2304 mL
60 mM 0.0410 mL 0.2051 mL 0.4101 mL 1.0253 mL
80 mM 0.0308 mL 0.1538 mL 0.3076 mL 0.7690 mL
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Pamapimod Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

Pamapimod449811-01-2Ro4402257 R1503Ro 4402257Ro-4402257R1503R 1503R-1503p38 MAPKAutophagyp38αp38βanti-inflammationRATNF-αIL-6LPSJNKIL-1βInhibitorinhibitorinhibit

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