SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively[1][2].
LY 235959 is a competitive N-methyl-D-aspartate (NMDA)-receptor antagonist. LY 235959 potentiates the anticonvulsant action of antiepileptics[1].
ISIS-2503, a 20-mer antisense oligonucleotide that inhibits Ha-Ras expression
Pamidronic acid is a drug used to treat a broad spectrum of bone absorption diseases.
CAM741 is a selective VCAM-1 translocation inhibitor. CAM741 selectively inhibits VCAM-1 expression by inhibiting its co-translational translocation within the lumen of the endoplasmic reticulum (ER). CAM741 can be used as a molecular tool and can also be used in the research of chronic inflammation and cancer[1][2].
ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC50 of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects[1][2].
Hyaluronan-IN-1 is a biological active peptide. (This 12 amino acids peptide is a hyaluronan inhibitor (HA), a high molecular weight glycosaminoglycan expressed abundantly in the extracellular matrix and on cell surfaces. This peptide shows specific binding to soluble, immobilized, and cell-associated forms of HA, and it inhibits leukocyte adhesion to HA substrates almost completely.)
D-Histidine monohydrochloride monohydrate is a histidine derivative[1].
Angiogenin Fragment (108-123) is a C-terminal segment 108-123 of Angiogenin that inhibits the enzymatic and biological activities of Angiogenin[1].
PROTAC BRD4 Degrader-2 is an efficacious PROTAC BRD4 degrader with an IC50 of 14.2 nM against BRD4 BD1[1].
Macbecin is a stable HSP90 inhibitor by binding to the ATP-binding site with an IC50 of 2 μM and a Kd of 0.24 μM. Macbecin exhibits antitumor and cytocidal activities[1].
Alsactide, a heptadecapeptide analogue, is an adrenocorticotropic hormone (ACTH) agonist. Alsactide can be used in research of central nervous system[1].
Sorbitan monododecanoate is a sorbitan ester surfactant. Sorbitan monododecanoate can be used as an excipient, such as nonionic surfactants, emulsifiers. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs[1][2].
SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.IC50 value: 7.2 (pKb) [1]Target: orexin OX1 receptor in vitro: SB-334867-A inhibited the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses (pK(B)=7.27+/-0.04 and 7.23+/-0.03 respectively, n=8), but had no effect on the UTP (3 microM)-induced calcium response in CHO-OX(1) cells. SB-334867-A (10 microM) also inhibited OX(2) mediated calcium responses (32.7+/-1.9% versus orexin-A) [1].in vivo: Single-unit recordings in anesthetized rats demonstrated the central effects of the selective orexin-1 receptor antagonist SB-334867 (2 mg/kg, intravenous), as it reversed the excitatory effects of orexin-A administration (6 microg, intracerebroventricular) on the activity of locus coeruleus (LC) cells [2]. The ICV injection of SB-334867 alone had no effect on the formalin-induced nociceptive behaviors. Pre-treatment with SB-334867 at a dose of 0.5 nmol significantly attenuated the analgesia induced by morphine (at dose 1.5mg/kg of morphine; interphase and phase 2B and at dose 3mg/kg of morphine just phase 2B of formalin test) [3]. Administered alone, SB-334867 (30 mg/kg, but not lower doses) significantly reduced food intake and most active behaviours (eating, grooming, sniffing, locomotion and rearing), while increasing resting. Pretreatment with SB-334867 dose-dependently blocked these effects of orexin-A, with significant antagonism evident at dose levels (3-10 mg/kg) below those required to produce intrinsic behavioural effects under present test conditions in rats [4].Toxicity: Acute systemic treatment with the selective orexin-1 (OX1R) antagonist SB-334867 reduces food intake in rats, an effect associated with an acceleration in behavioural satiety and unrelated to gross behavioural disruption, alterations in palatability, or toxicity.
Ac-Gly-Ala-Val-Ile-Leu-Arg-Arg-NH2 is a conical peptide with a nanodonut structure[1].
Alisol A 23-acetate is a natural product that can be isolated from Rhizoma Alismatis[1].
Ceftazidime pentahydrate (GR20263 pentahydrate) is a third generation cephalosporin administered intravenously or intramuscularly. Ceftazidime pentahydrate has a broad spectrum of in vitro activity against Gram-positive and Gram-negative aerobic bacteria. Ceftazidime pentahydrate is particularly active against Enterobacteriaceae (including beta-lactamase-positive strains) and is resistant to hydrolysis by most beta-lactamases[1].
β-Cyclogeraniol is a natural odour compound[1].
N-Acetyldopamine dimer-1 is a 2-(3',4'-dihydroxyphenyl)-1,4-benzodioxane derivative. N-Acetyldopamine dimer-1 is optically active, can be isolated from crude drug "Zentai," a cast-off shell of the cicada of Cryptotympana sp. (Cicadidae)[1].
Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts[1].
Chemerin-9 (149-157), the nonapeptide (149)YFPGQFAFS(157) (chemerin-9), corresponding to the C terminus of processed chemerin, retains most of the activity of the full-size protein, with regard to agonism toward the chemerinR[1].
Amino-PEG5-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Sugereoside is a bitter diterpene glucoside. Sugereoside can be isolated from leaves of Ilex sugerokii var[1].
Lycorenine is an alkaloid that has vasodepressor action. Lycorenine also exhibits anticancer and antibacterial activities[1][2][3].
UK 14,304 is a full α2-adrenergic receptor (α2-AR) agonist.Target: α2-adrenergic Receptor[3H]UK 14,034 is a full agonist at alpha 2-adrenergic receptors. [3H]UK 14,304 labels at least 2 specific binding sites in human brain that both have the characteristics of an alpha 2-adrenergic binding site. GTP decreases agonist binding at both of these sites, but with different potencies at each site [1-3].
NADP disodium salt is a participant coenzyme in aerobic and anaerobic oxidations.
Boc-N-Me-DL-Val-OH is a valine derivative[1].
Suptavumab (REGN2222) is a human monoclonal antibody. Suptavumab can bind and block a conserved epitope on RSV A and B subtypes. Suptavumab can be used for the research of RSV infection[1][2].
Fmoc-Val-Cit-PAB-MMAE consists the ADCs linker (Fmoc-Val-Cit-PAB) and potent tubulin inhibitor (MMAE), Fmoc-Val-Cit-PAB-MMAE is an antibody drug conjugate.
Coenzyme Q10-d6 is deuterium labeled Coenzyme Q10. Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.