INCB3344

Product Name: INCB3344
CAS No.: 1262238-11-8
Chemical Name: INCB3344
Synonyms: INCB3344 ，S8220;INCB 3344;INCB-3344;INCB3344, 10 mM in DMSO;CC chemokine receptor,INCB3344,CCR,Inhibitor,inhibit,INCB-3344,INCB 3344;N-(2-(((3R,4R)-1-(trans-4-(Benzo[d][1,3]dioxol-5-yl)-4-hydroxycyclohexyl)-4-ethoxypyrrolidin-3-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide;rel-N-[2-[[(3R,4R)-1-[trans-4-(1,3-Benzodioxol-5-yl)-4-hydroxycyclohexyl]-4-ethoxy-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide;Benzamide, N-[2-[[(3R,4R)-1-[trans-4-(1,3-benzodioxol-5-yl)-4-hydroxycyclohexyl]-4-ethoxy-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)-, rel-
CBNumber: CB52624184
Molecular Formula: C29H34F3N3O6
Formula Weight: 577.59
MOL File: 1262238-11-8.mol

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INCB3344 Property

Boiling point:: 736.3±60.0 °C(Predicted)
Density: 1.38±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: ≥25.9 mg/mL in DMSO; insoluble in H2O; ≥89.8 mg/mL in EtOH
form: solid
pka: 12.94±0.46(Predicted)
color: White to yellow

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Safety

WGK Germany: WGK 3
Storage Class: 11 - Combustible Solids

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML3924
Product name: INCB3344
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $192
Updated: 2026/03/19

Sigma-Aldrich

Product number: SML3924
Product name: INCB3344
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $771
Updated: 2026/03/19

Cayman Chemical

Product number: 28433
Product name: INCB 3344
Packaging: 1mg
Price: $93
Updated: 2024/03/01

Cayman Chemical

Product number: 28433
Product name: INCB 3344
Packaging: 10mg
Price: $638
Updated: 2024/03/01

Cayman Chemical

Product number: 28433
Product name: INCB 3344
Packaging: 5mg
Price: $343
Updated: 2024/03/01

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INCB3344 Chemical Properties,Usage,Production

Description

INCB 3344 is an antagonist of chemokine (C-C motif) receptor 2 (CCR2; IC₅₀ = 10 nM in WEHI-274 murine monocytes). It is selective for CCR2 over a panel of G protein-coupled receptors, including CCR1 and CCR5, with IC₅₀s values greater than 1 μM. INCB 3344 inhibits chemotaxis of WEHI-274 cells induced by chemokine (C-C motif) ligand 2 (CCL2; IC₅₀ = 10 nM) and CCL2-induced phosphorylation of ERK in WEHI-274 cells. It inhibits monocyte influx in a mouse model of peritonitis induced by thioglycolate when administered at doses of 60 and 100 mg/kg. INCB 3344 (30, 50, and 100 mg/kg twice per day) decreases the expression of CCR2 mRNA in the ear and reduces ear swelling in a mouse model of delayed-type hypersensitivity reaction. It prevents increases in or reduces macrophage levels in the spinal cord when administered at a dose of 100 mg/kg per day beginning the day of immunization or seven days following immunization, respectively, in a mouse model of experimental autoimmune encephalomyelitis (EAE). It also reduces disease incidence and severity in the same model and reduces disease severity in a rat model of adjuvant-induced arthritis. INCB 3344 reduces macrophage infiltration to the kidney and improves renal function in a mouse model of polycystic kidney disease.

Uses

INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.

in vivo

When administered intravenously to CD-1 mice, INCB3344 exhibits a high clearance and a moderate volume of distribution, resulting in a short half life of 1 h. Despite its high clearance, however, good oral exposure is achieved, with an AUC at 2664 nM h at a dose of 10 mg/kg. The oral bioavailability is 47%. By comparison, slightly better oral exposure (AUC=3888 nM h) is obtained when administered orally to Balb/c mice at the same dose. This PK property, couple with its potent anti-mCCR2 activity and good selectivity, makes this compound suitable for model studies in rodents^[1]. INCB3344 prevents Deoxycorticosterone acetate/salt-induced changes in vascular expression of CCR2. In a separate series of experiments, CCR2 expression is elevated (≈1.5-fold higher) in aortas from mice that receive INCB3344 from days 7 to 21 of the Deoxycorticosterone acetate/salt treatment period compare with sham animals; however, this level of CCR2 expression is significantly lower than that observed in the vehicle-treated group (P<0.05, n=6). Likewise, increased expression of its receptor ligand CCL2 in Deoxycorticosterone acetate/salt-treated mice is blunted in mice receiving INCB3344 (P<0.05, n=6). By contrast, levels of CCL7, CCL8, and CCL12 are elevated to similar extents in Deoxycorticosterone acetate/salt-treated mice receiving vehicle or INCB3344^[3].

IC 50

hCCR2: 5.1 nM (IC₅₀); mCCR2: 9.5 nM (IC₅₀)

References

[1]. brodmerkel c m, huber r, covington m, et al. discovery and pharmacological characterization of a novel rodent-active ccr2 antagonist, incb3344[j]. the journal of immunology, 2005, 175(8): 5370-5378.

INCB3344 Preparation Products And Raw materials

Raw materials

Preparation Products

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INCB3344 Suppliers

China 52 United States 8 Global 60

Shanghai Boyle Chemical Co., Ltd.

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Haoyuan Chemexpress Co., Ltd.

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MedChemexpress LLC

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ShangHai Caerulum Pharma Discovery Co., Ltd.

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DKMbiochem.Co. Ltd

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LETOPHARM LIMITED

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Shanghai Lollane Biological Technology Co.,Ltd.

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SPIRO PHARMA

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Codow Chemical Co.,Ltd.

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Shanghai EFE Biological Technology Co., Ltd.

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1262238-11-8, INCB3344Related Search:

INCB 3344;INCB-3344

rel-N-[2-[[(3R,4R)-1-[trans-4-(1,3-Benzodioxol-5-yl)-4-hydroxycyclohexyl]-4-ethoxy-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide

Benzamide, N-[2-[[(3R,4R)-1-[trans-4-(1,3-benzodioxol-5-yl)-4-hydroxycyclohexyl]-4-ethoxy-3-pyrrolidinyl]amino]-2-oxoethyl]-3-(trifluoromethyl)-, rel-

CC chemokine receptor,INCB3344,CCR,Inhibitor,inhibit,INCB-3344,INCB 3344

INCB3344, 10 mM in DMSO

N-(2-(((3R,4R)-1-(trans-4-(Benzo[d][1,3]dioxol-5-yl)-4-hydroxycyclohexyl)-4-ethoxypyrrolidin-3-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide

INCB3344 ，S8220

1262238-11-8

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