MW 506.5 Da, Purity >99%. Potent 5-HT2A receptor antagonist (Ki = 7.1 nM for inhibition of [3H] ketanserin binding in rat cortex). Additionally blocks α1 adrenoceptors (Ki values are 5.5 and 84 nM at α1 and α2, respectively). Acts as a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) (Ki values are 220 and 555 nM at rat SERT and NET, respectively). Antidepressant.
2700049B16Rik, 3110031N04Rik, ACLS, AI838772, AIS, ANDR_HUMAN, AR, AR8, ARO, ARO1, AW493413, Androgen nuclear receptor variant 2, Androgen receptor, Androgen receptor (dihydrotestosterone receptor; testicular feminization; spinal and bulbar muscular atrophy; Kennedy disease), Aromatase, Atherosclerosis, susceptibility to, included, BK channel, BK channel beta subunit, BK channel subunit beta-1, BK channel subunit beta-2, BK channel subunit beta-4, BKCA alpha, BKCA alpha subunit, BKTM, BKbeta, BKbeta1, BKbeta2, BKbeta4, BXR, CAPC, CP19A_HUMAN, CPV1, CYAR, CYP19, CYPXIX, Calcium activated potassium channel beta 4 subunit, Calcium activated potassium channel subfamily M subunit beta 1, Calcium activated potassium channel subfamily M subunit beta 2, Calcium activated potassium channel subfamily M subunit beta 4, Calcium-activated potassium channel, Calcium-activated potassium channel subunit alpha-1, Calcium-activated potassium channel subunit beta, Calcium-activated potassium channel subunit beta-1, Calcium-activated potassium channel subunit beta-2, Calcium-activated potassium channel subunit beta-4, Charybdotoxin receptor subunit beta-1, Charybdotoxin receptor subunit beta-2, Charybdotoxin receptor subunit beta-4, Cyp19a1, Cytochrome P-450AROM, Cytochrome P450 19A1, Cytochrome P450, family 19, subfamily A, polypeptide 1, Cytochrome P450, subfamily XIX (aromatization of androgens), Cytokeratin-associated protein in cancer, DHTR, DKFZp686N23123, DNA binding protein, Dihydro testosterone receptor, Dihydrotestosterone receptor (DHTR), Drosophila slowpoke like, ER, ER-alpha, ER-beta, ERR a, ERR-alpha, ERR1 protein, ERR1_HUMAN, ER[a], ER[b], ESR, ESR B, ESR BETA, ESR1_HUMAN, ESRA, ESRL 1, ESRR A, ESTR B, Eag-related protein 1, Era, Erb, Erb2, Estr, Estra, Estradiol Receptor alpha, Estradiol Receptor beta, Estradiol receptor, Estrogen Receptor 1, Estrogen Receptor 2, Estrogen receptor, Estrogen receptor 1 (alpha), Estrogen receptor 2 (ER beta), Estrogen receptor 2 ER beta, Estrogen receptor alpha, Estrogen receptor beta 4, Estrogen receptor related 1, Estrogen receptor-like 1, Estrogen resistance, included, Estrogen synthase, Estrogen synthetase, Estrogen-related receptor alpha, Estrra, Ether a go go related potassium channel protein, Ether-a-go-go-related gene potassium channel 1, Ether-a-go-go-related protein 1, FLJ11090, GCCR, GCPS, GCRST, GCR_HUMAN, GLI Kruppel family member GLI 3, GLI Kruppel family member GLI3 (Greig cephalopolysyndactyly syndrome), GLI family zinc finger 3, GLI3 C-terminally truncated form, GLI3 form of 190 kDa, GLI3 form of 83 kDa, GLI3 full length protein, GLI3-190, GLI3-83, GLI3FL, GLI3_HUMAN, GR, Glioma associated oncogene family zinc finger 3, Glucocorticoid receptor, Grl1, H-ERG, HDL cholesterol, augmented response of, to hormone replacement, included, HUMARA, HYSP1, Hbeta1, Hbeta2, Hbeta3, Hbeta4, IMD42, K(VCA)alpha, K(VCA)beta, K(VCA)beta-1, K(VCA)beta-2, K(VCA)beta-4, KCMA1_HUMAN, KCMB1_HUMAN, KCMB2_HUMAN, KCMB4_HUMAN, KCNH2_HUMAN, KCNMA, KCNMA1, KCNMB 1, KCNMB 2, KCa1.1, KD, Kennedy disease (KD), Kv11.1, LQT 2, LRC26_HUMAN, Large conductance Ca2+ activated K+ channel beta 1 subunit, Large conductance Ca2+ activated K+ channel beta2 subunit, Large conductance calcium activated potassium channel beta 2 subunit, Large conductance calcium dependent potassium ion channel beta 4 subunit, Leucine-rich repeat-containing protein 26, Lrrc26, MGC104252, MGC104309, MGC112732, MGC129539, MGC22431, MGC57945, Maxi K channel, Maxi K channel beta subunit, Maxi K channel subunit beta-1, Maxi K channel subunit beta-2, Maxi K channel subunit beta-4, Maxi Potassium channel alpha, MaxiK, MaxiK channel beta 2 subunit, Microsomal monooxygenase, Myocardial infarction, susceptibility to, included, NF-E2-related factor 2, NF2L2_HUMAN, NR1F3, NR1I2_HUMAN, NR3A1, NR3A2, NR3B1, NR3C3, NR3C4, NRF2, Nfe2l2, Nuclear factor, Nuclear factor (erythroid derived 2) like 2, Nuclear factor erythroid 2-related factor 2, Nuclear factor erythroid derived 2 like 2, Nuclear receptor ROR-gamma, Nuclear receptor RZR-gamma, Nuclear receptor subfamily 1 group F member 3, Nuclear receptor subfamily 1 group I member 2, Nuclear receptor subfamily 3 group A member 1, Nuclear receptor subfamily 3 group A member 2, Nuclear receptor subfamily 3 group B member 1, Nuclear receptor subfamily 3 group C member 1, Nuclear receptor subfamily 3 group C member 3, Nuclear receptor subfamily 3 group C member 4, Nuclear receptor subfamily 3 group C member 4 (NR3C4), ONR 1, OTTHUMP00000017718, OTTHUMP00000017719, OTTHUMP00000162543, OTTHUMP00000198350, OTTHUMP00000215173, OTTHUMP00000215174, OTTHUMP00000215175, Oncogene GLI3, Orphan nuclear receptor PAR 1, Orphan nuclear receptor PXR, P 450AROM, PAP A, PAPB, PAR, PAR q, PGR, PPD IV, PR, PRA, PRB, PRGR_HUMAN, PRR, Potassium channel HERG, Potassium large conductance calcium activated channel subfamily M beta member 1, Potassium large conductance calcium activated channel subfamily M beta member 2, Potassium large conductance calcium activated channel subfamily M beta member 4, Potassium voltage gated channel subfamily H (eag related) member 2, Potassium voltage-gated channel subfamily H member 2, Pregnane X receptor, Progesterone receptor, Progestin receptor form A, Progestin receptor form B, RAR related orphan nuclear receptor variant 2, RAR related orphan receptor C, isoform a, RAR related orphan receptor gamma, RAR-related orphan receptor C, RNESTROR, RORG_HUMAN, RP24-311F12.2, RZR GAMMA, RZRG, Retinoic acid binding receptor gamma, Retinoid-related orphan receptor-gamma, Rorc, SAKCA, SBMA, SCAN1, SLO, SMAX1, SQT1, SXR, Slo homolog, Slo-alpha, Slo-beta, Slo-beta-1, Slo-beta-2, Slo-beta-4, Slo1, Slowpoke homolog, Spinal and bulbar muscular atrophy, Spinal and bulbar muscular atrophy (SBMA), Steroid and xenobiotic receptor, Steroid hormone receptor ERR1, TFM, TOR, TYDP, TYDP1_HUMAN, Testicular Feminization (TFM), Transcriptional activator GLI3, Transcriptional repressor GLI3R, Tyr-DNA phosphodiesterase 1, Tyrosyl-DNA phosphodiesterase 1, Voltage gated potassium channel, subfamily H, member 2, Voltage-gated potassium channel subunit Kv11.1, Zinc finger protein GLI 3, androgen receptor splice variant 4b, bA350O14.10, cytokeratin-associated protein, eag homolog, erythroid derived 2, estrogen receptor related receptor alpha, flavoprotein-linked monooxygenase, glucocorticoid nuclear receptor variant 1, hERG-1, hERR1, hSlo, hslo beta, like 2, nr3c1, nuclear factor erythroid 2 like 2, nuclear receptor subfamily 3, group C, member 1 (glucocorticoid receptor), pregnane X nuclear receptor variant 2, subfamily M subunit alpha-1, subfamily M subunit beta-1, subfamily M subunit beta-2, subfamily M subunit beta-4
MW 506.5 Da, Purity >99%. Potent 5-HT2A receptor antagonist (Ki = 7.1 nM for inhibition of [3H] ketanserin binding in rat cortex). Additionally blocks α1 adrenoceptors (Ki values are 5.5 and 84 nM at α1 and α2, respectively). Acts as a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) (Ki values are 220 and 555 nM at rat SERT and NET, respectively). Antidepressant.
Soluble in DMSO to 25 mM.
Soluble in ethanol to 10 mM.
Soluble in 1 eq. HCl to 10 mM.
Potent 5-HT2A receptor antagonist (Ki = 7.1 nM for inhibition of [3H] ketanserin binding in rat cortex). Additionally blocks α1 adrenoceptors (Ki values are 5.5 and 84 nM at α1 and α2, respectively). Acts as a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) (Ki values are 220 and 555 nM at rat SERT and NET, respectively). Antidepressant.
The biological targets listed are diverse in their mechanical roles. Glucocorticoid Receptor Progesterone Receptor and Estrogen Receptor collectively known as nuclear receptors are involved in regulating gene expression. Expressed widely in various tissues these receptors have masses around 94 kDa 99 kDa and 67 kDa respectively. Gli3 is a transcription factor important in developmental processes with widespread expression noted during embryonic development. The Maxi Potassium channel alpha (SLO) and associated beta subunits (KCNMB1 KCNMB2 KCNMB4 and LRRC26) contribute to large conductance calcium-activated potassium channels in excitable cells. TDP1 plays a role in DNA repair and is localized to the nucleus while Aromatase involved in estrogen synthesis appears mainly in the adrenal glands and gonads. Nrf2 (Nuclear factor erythroid 2-related factor 2) acts as a transcription factor for antioxidant response. The Androgen Receptor similar to other nuclear receptors plays a role in transcription regulation within tissues like prostate and muscle.
These proteins and receptors participate in key physiological processes. Nuclear receptors like the Glucocorticoid Progesterone and Estrogen Receptors regulate reproduction metabolism and immune response by controlling the expression of target genes. The Androgen Receptor interact structurally with coactivators within the nucleus to mediate their effects. Aromatase facilitates estrogen biosynthesis impacting reproductive tissues and bone integrity. Gli3 influences the formation of limbs and organs by regulating Hedgehog signaling. Maxi Potassium channels with their alpha and beta subunits influence muscle contraction and neurotransmitter release by modulating membrane potential. TDP1 participates in the repair of DNA double-strand breaks ensuring genomic stability. Nrf2 responds to oxidative stress forming a complex with Keap1 under non-stress conditions initiating protective gene transcription when activated.
These proteins integrate into important cellular mechanisms. Nuclear receptors including Glucocorticoid and Estrogen Receptors are central to the steroid hormone signaling pathway. This pathway coordinates with the Mitogen-Activated Protein Kinase (MAPK) pathway to modulate cellular growth and differentiation. Gli3 functioning in the Sonic Hedgehog pathway interacts with Patched and Smoothened proteins that affect developmental processes. Maxi Potassium channels play roles in the regulation of calcium signaling pathways interacting with proteins like CaM (Calmodulin). Aromatase contributes to the estrogen synthesis pathway overlapping with steroidogenesis involving StAR (Steroidogenic acute regulatory protein). Nrf2 operates in the cellular antioxidant defense pathway modulating oxidative stress responses in interaction with proteins like BACH1.
These targets have significant medical implications. Aberrations in Glucocorticoid and Estrogen Receptors relate to hormone-sensitive cancers such as breast and prostate cancer often co-implicating the Androgen Receptor. Gli3 mutations result in developmental disorders like Greig cephalopolysyndactyly syndrome. Dysregulation of Aromatase leads to estrogen-dependent diseases affecting bone health and conditions like endometriosis. Maxi Potassium channel defects cause neurological disorders through abnormal neuronal firing patterns. TDP1 deficiencies associate with neurodegenerative conditions such as spinocerebellar ataxia. Nrf2 dysfunctions contribute to the pathogenesis of chronic diseases like cancer and neurodegeneration indicating overlapping roles with proteins in oxidative stress pathways.
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2D chemical structure image of ab120587, Nefazodone hydrochloride, 5-HT2A antagonist
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