The G-coupled receptor superfamily includes the CRFR, also known as the corticotropin-releasing factor receptor (CRHR). There are two distinct receptor subtypes—CRF1 receptor and CRF2 receptor—as well as numerous splice variants for each receptor subtype. Urocortin 1 (Ucn 1) binds to both CRF1 and CRF2 receptors with high affinity, whereas CRF itself has a stronger affinity for CRF1 receptors.Urocortins 2 and 3 both preferentially bind to CRF2 receptors.
Two distinct genes that code for different subtypes of the CRF receptor exhibit a variety of alternative pre-mRNA splicing patterns, leading to a variety of variants resulting from partial or complete exon deletions or insertions. Regarding the nine human CRF1 isoforms (CRF1a-i) that have been described, CRF1a is the primary functional wild-type receptor, whereas the other isoforms may modulate CRF signaling. Three functionally active splice variants of the CRF2, designated CRF2a-c, have been identified in humans.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V3636 | Verucerfont | 885220-61-1 | Verucerfont (also known as GSK561679 and NBI77860) is a novel and potent antagonist of corticotropin-releasing factor receptor 1 (CRF1) with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively. |
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V74554 | α-Helical CRF(9-41) | 90880-23-2 | α-Helical CRF(9-41) is a competitive CRF2 receptor antagonist (inhibitor) with a KB of approximately 100 nM. |
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V69050 | α-Helical CRF(9-41) TFA | α-Helical CRF(9-41) TFA is a competitive CRF2 receptor antagonist (inhibitor) with a KB of approximately 100 nM. |
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