HS271 - ≥99% , CAS No.2410393-15-4

CAS: 2410393-15-4 Cat. No.: H649344 분자식: C₂₁H₂₄F₃N₅O₂ 분자량: 435.44 PubChem CID: 146386401

등급 & 순도 ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

개요

HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC 50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties

In Vivo

HS271 (15-150 mg/kg) displays robust in vivo antiinflammatory efficacy as evaluated in rat models of LPS induced TNFα production collageninduced arthritis . HS271 exhibits a t 1/2 of 3.3 h and C max of 2107 ng/mL . HS271 is stable in liver microsome assays across other species, including rat, mouse, monkey, and human . HS271 exhibits oral bioavailability of 67.3%, 58.2%, 14.4&% and 49% in mouse, rat, dog and monkey, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: A rat model of collagen induced arthritis (CIA) . Dosage: 15, 50, 150 mg/kg. Administration: PO, once daily. Result: Led to a significant reduction in paw swelling as compared to vehicle control, with a minimum effective dose at 15 mg/kg QD. Notably, at 150 mg/kg QD, HS271 eliminated the paw swelling.

Form:Solid

IC50& Target:IRAK4 7.2 μM (IC 50 )

사양

사양 및 순도

≥99%

생화학 및 생리적 메커니즘

HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC 50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties.

보관 조건

Store at -20°C

배송

Ice chest + Ice pads

이 제품은 콜드 체인 배송이 필요합니다.지상 및 기타 경제 서비스는 사용할 수 없습니다.

작업 유형

INHIBITOR

순수함

≥99%

이름과 식별자

정식 스마일

CC(C)(C1=CC2=NN(C=C2C=C1NC(=O)C3=NC(=CC=C3)C(F)(F)F)CCN(C)C)O

IUPAC Name

N-[2-[2-(dimethylamino)ethyl]-6-(2-hydroxypropan-2-yl)indazol-5-yl]-6-(trifluoromethyl)pyridine-2-carboxamide

InChIKey

QAOWCAZEVIIQTF-UHFFFAOYSA-N

INCHI

1S/C21H24F3N5O2/c1-20(2,31)14-11-16-13(12-29(27-16)9-8-28(3)4)10-17(14)26-19(30)15-6-5-7-18(25-15)21(22,23)24/h5-7,10-12,31H,8-9H2,1-4H3,(H,26,30)

이성체 SMILES

CC(C)(C1=CC2=NN(C=C2C=C1NC(=O)C3=NC(=CC=C3)C(F)(F)F)CCN(C)C)O

PubChem CID

146386401

분자량

435.44

관련 대상(인간)

IRAK4 Tchem Interleukin-1 receptor-associated kinase 4 (1 Activities)

Discover Target: IRAK4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin HERG (29587 Activities)

Discover Target: KCNH2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP2C8 Tchem Cytochrome P450 2C8 (1492 Activities)

Discover Target: CYP2C8

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)

Discover Target: CYP2D6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)

Discover Target: CYP1A2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)

Discover Target: CYP2C9

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)

Discover Target: CYP2C19

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)

Discover Target: CYP3A4

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

IRAK1 Tchem Interleukin-1 receptor-associated kinase 1 (1749 Activities)

Discover Target: IRAK1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

IRAK4 Tchem Interleukin-1 receptor-associated kinase 4 (5917 Activities)

Discover Target: IRAK4

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP2B6 Tchem Cytochrome P450 2B6 (1338 Activities)

Discover Target: CYP2B6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

작용 메커니즘

화학 및 물리적 특성

• 용해성: DMSO : 100 mg/mL (229.65 mM; Need ultrasonic)

자주 묻는 질문

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2410393-15-4, the molecular formula is C21H24F3N5O2, and the molecular weight is 435.44 g/mol. InChIKey QAOWCAZEVIIQTF-UHFFFAOYSA-N.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.