MW 445 Da, Purity >99%. Potent and selective CCR1 antagonist (IC50 = 8.4 μM). Ki values are 0.04 nM (CCR1) and >10 nM (CCR5, CXCR2 and CXCR4). Displays inverse agonist activity for US28, a HCMV-encoded receptor. Able to produce concentration-dependent inhibition of MIP-1α and Ca2+ mobilization.
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Key facts
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 445 Da
- Molecular formula
- C28H29ClN2O
- PubChem identifier
- 9889700
- Nature
- Synthetic
Alternative names
C-C CKR-1, C-C CKR-3, C-C chemokine receptor type 1, C-C chemokine receptor type 3, CC chemokine receptor 3, CCR1_HUMAN, CCR3_HUMAN, CD 191, CD 193, CD191 antigen, CD193 antigen, CK R3, CKR 1, CKR 3, CKR3, CMKB R3, CMKBR 1, CMKBR1L2, CMKR 1, Chemokine (C C motif) receptor 1, Chemokine (CC) receptor 1 like 2, Chemokine C C motif receptor 1, Chemokine CC motif receptor 3, Chemokine receptor 3, D(2) dopamine receptor, D2 dopamine receptor, D2DR, D2R, DRD2_HUMAN, Dopamine D2 receptor, Dopamine receptor D2, Eosinophil CC chemokine receptor 3, Eosinophil eotaxin receptor, Eotaxin receptor, HM145, LD78 receptor, MGC102841, MIP-1alpha-R, MIP1 Alpha RL2, Macrophage inflammatory protein 1 alpha /Rantes receptor, Macrophage inflammatory protein 1 alpha receptor like 2, Macrophage inflammatory protein 1-alpha receptor, Mip 1a R, RANTES receptor, RANTES-R, SCYAR1, b-chemokine receptor, chemokine (C-C motif) receptor 3
Recommended products
MW 445 Da, Purity >99%. Potent and selective CCR1 antagonist (IC50 = 8.4 μM). Ki values are 0.04 nM (CCR1) and >10 nM (CCR5, CXCR2 and CXCR4). Displays inverse agonist activity for US28, a HCMV-encoded receptor. Able to produce concentration-dependent inhibition of MIP-1α and Ca2+ mobilization.
Key facts
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 445 Da
- Molecular formula
- C28H29ClN2O
- PubChem identifier
- 9889700
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 100 mM.
Soluble in ethanol to 50 mM.
- Biochemical name
- 5-[4-(4-Chlorophenyl)-4-hydroxy-1-piperidyl]-2,2-diphenyl-pentanenitrile
- Biological description
Potent and selective CCR1 antagonist (IC50 = 8.4 μM). Ki values are 0.04 nM (CCR1) and >10 nM (CCR5, CXCR2 and CXCR4). Displays inverse agonist activity for US28, a HCMV-encoded receptor. Able to produce concentration-dependent inhibition of MIP-1α and Ca2+ mobilization.
- Canonical SMILES
- C1CN(CCC1(C2=CC=C(C=C2)Cl)O)CCCC(C#N)(C3=CC=CC=C3)C4=CC=CC=C4
- InChI
- InChI=1S/C28H29ClN2O/c29-26-14-12-25(13-15-26)28(32)17-20-31(21-18-28)19-7-16-27(22-30,23-8-3-1-4-9-23)24-10-5-2-6-11-24/h1-6,8-15,32H,7,16-21H2
- InChIKey
- MEEJEEVTIVAOJP-UHFFFAOYSA-N
- IUPAC name
- 5-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-2,2-diphenylpentanenitrile
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- +4°C
- Appropriate long-term storage conditions
- +4°C
- Storage information
- Store under desiccating conditions, The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
CCR3 (C-C chemokine receptor type 3) and CCR1 (C-C chemokine receptor type 1) belong to the chemokine receptor family which act as signaling proteins involved in immune responses. The CCR3 receptor has an approximate mass of 41 kDa while CCR1 is around 42 kDa. These receptors are expressed on various immune cells such as eosinophils and basophils. The dopamine D2 receptor also known as DRD2 has a mass of approximately 50 kDa and is expressed mainly in the central nervous system particularly in dopaminergic neurons. All three play significant roles through G-protein coupled receptor (GPCR) mechanisms.
- Biological function summary
The CCR3 receptor mediates the migration and activation of inflammatory cells heavily involved in allergic responses. CCR1 also facilitates cell movement and acts in inflammatory processes often working in conjunction with chemokines such as CCL5. The dopamine D2 receptor influences neurotransmission and plays critical roles in modulating physiological functions like locomotion and behavior. While unrelated in function these proteins act through receptor complexes involving second messengers to relay signals inside cells.
- Pathways
CCR3 participates in the chemokine signaling pathway integral for directing cell traffic and maintaining tissue homeostasis. It interacts with proteins like CXCR4 in immune regulation. CCR1 also engages in chemokine signaling having significant interactions within inflammatory pathways. The dopamine D2 receptor is a part of dopaminergic signaling pathways and interacts closely with proteins like G-proteins particularly influencing the cyclic AMP production in neurons.
- Associated diseases and disorders
CCR3 and CCR1 connect to conditions like asthma and rheumatoid arthritis where inflammatory mechanisms are prominent. CCR3 is linked with eosinophilic inflammation in asthma. The dopamine D2 receptor is associated with neurological disorders such as schizophrenia and Parkinson's disease where dopaminergic regulation is disrupted. Through shared pathways CCR3 CCR1 and DRD2 align with various other proteins influencing disease progression and treatment strategies.
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1 product image
Chemical Structure - BX 513 hydrochloride, CCR1 antagonist (ab120811)
2D chemical structure image of ab120811, BX 513 hydrochloride, CCR1 antagonist
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